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Formulation and characterization of nanostructured lipid carrier encapsulated Zingiber zerumbet oil using ultrasonication technique
Abstract
This study presents the formulation of nanostructured lipid carrier encapsulated Zingiber zerumbet oil (NLC-ZZ) using ultrasonication technique. NLC is the blend of solid lipid, liquid lipid and surfactant for encapsulation of poor water soluble actives. The NLC-ZZ formulation was characterized with respect to particle size, polydispersity index (PDI), zeta-potential, encapsulation efficiency and physical morphology. The NLC-ZZ formulation had an average diameter of 96.59 nm, PDI of 0.192, zeta-potential of-39.88 mV, and encapsulation efficiency of 90%, respectively. The NLC formulation for Zingiber zerumbet oil encapsulation has been successfully developed and is suitable for transdermal delivery system due to their nano-size and stability.
... The NLCs also improved the stability of silymarin [72]. Rosli et al. (2015) reported that NLCs loaded with Zingiber zerumbet oil, a phytochemical found in Zingiber zerumbet (pinecone or shampoo ginger), were stable and suitable for transdermal delivery systems [73]. Zingiber zerumbet oil itself was found to have anti-P. ...
... The NLCs also improved the stability of silymarin [72]. Rosli et al. (2015) reported that NLCs loaded with Zingiber zerumbet oil, a phytochemical found in Zingiber zerumbet (pinecone or shampoo ginger), were stable and suitable for transdermal delivery systems [73]. Zingiber zerumbet oil itself was found to have anti-P. ...
Acne vulgaris (acne) is one of the most common dermatological problems affecting adolescents and young adults. Although acne may not lead to serious medical complications, its psychosocial effects are tremendous and scientifically proven. The first-line treatment for acne is topical medications composed of synthetic compounds, which usually cause skin irritation, dryness and itch. Therefore, naturally occurring constituents from plants (phytochemicals), which are generally regarded as safe, have received much attention as an alternative source of treatment. However, the degradation of phytochemicals under high temperature, light and oxygen, and their poor penetration across the skin barrier limit their application in dermatology. Encapsulation in lipid nanoparticles is one of the strategies commonly used to deliver drugs and phytochemicals because it allows appropriate concentrations of these substances to be delivered to the site of action with minimal side effects. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are promising delivery systems developed from the combination of lipid and emulsifier. They have numerous advantages that include biocompatibility and biodegradability of lipid materials, enhancement of drug solubility and stability, ease of modulation of drug release, ease of scale-up, feasibility of incorporation of both hydrophilic and lipophilic drugs and occlusive moisturization, which make them very attractive carriers for delivery of bioactive compounds for treating skin ailments such as acne. In this review, the concepts of SLNs and NLCs, methods of preparation, characterization, and their application in the encapsulation of anti-acne phytochemicals will be discussed.
... Zingiber Officinale oil incorporated in nanostructured lipid carrier (ZO-NLC) was prepared according to the method reported by Rosli et al. (2015) with some modifications [20]. Tween® 80 was chosen as the surfactant. ...
... Zingiber Officinale oil incorporated in nanostructured lipid carrier (ZO-NLC) was prepared according to the method reported by Rosli et al. (2015) with some modifications [20]. Tween® 80 was chosen as the surfactant. ...
Nowadays, nanostructured lipid carrier has been employed in pharmaceutics, nutraceuticals and biomedical formulations also other purposes. The aim of this study was to estimates the effect of high pressure homogenizer on the properties of zingiber officinale loaded nanostructured lipid carrier especially on size of particle and polydispersity index. Experiments were constructed using high pressure homogenizer by applying certain homogenizing pressure and cycle. The independent variables were homogenization pressure (0–2000 bar) and cycle (1-9) and the analysed responses were particles size and polydispersity index. The increase in the homogenization pressure up to 1300 bar and six cycle decreased the emulsion droplet size. However, the use of pressures above that pressure and cycle resulted in the formation of droplets with larger size.
... Surfactant is one of a method to improve the stability of a nanofluid. Surfactant or dispersant is a popular and economical method to enhance nanofluids' stability by affecting the mixture's surface characteristics [1][2][3]. Surfactants act as barriers and reduce the interfacial tension between suspended particles and the based fluid. It makes the suspension more stable by increasing the repulsive forces and the zeta potential. ...
A surfactant is an efficient approach for increasing the stability of nanofluids. However, excessive surfactant degrades the hybrid nanofluid's outstanding thermal conductivity. Additionally, there was only a little research on optimising the amount of surfactant used in nanofluids depending on their thermal conductivity. As a result, it is critical to ensure that the created nanofluid is stable without impairing thermal conductivity. The optimisation was carried out in this study utilising Design Expert 11. Surfactant ratios and the mixing ratio of hybrid nanofluid were employed as variables, while thermal conductivity was used as the response. Additionally, the concentration and temperature of the hybrid nanofluid remained constant at 0.5 vol% and 40 °C, respectively. The results indicate that a 1:10 ratio of surfactant to TiO2 is the optimal proportion for the generated TiO2-GNP hybrid nanofluid. The correct amount of surfactant results in a hybrid nanofluid with high thermal conductivity and good stability.
... NLC are fabricated by mixing solid lipids with spatially incompatible lipids leading to nanoparticulate structures with improved drug loading and controllable release properties [13]. To obtain NLC, there are several methods of preparation, microemulsions [14], high-shear homogenization/HSH [15,16], high-pressure homogenization/HPH [17,18], sonication [19], solvent diffusion [20] etc. Out of the numerous methods reported to prepare NLC, melting emulsification coupled with HPH is the most simple and preferred method [18,21]. ...
The scope of this research was to identify optimal compositions for both lipid and aqueous phases, suitable for obtaining nanostructured lipid carriers (NLCs) based on vegetable oils-primrose oil (Po) and soybean oil (So)-with average dimensions of about 200 nm and to evaluate their physical stability by determining the mean particle size (Zave) and zeta potential (ξ) at different time intervals (3 days, 1÷4 weeks and 60 days). Results showed that the composition of 2.5% surfactant mixture, in a weight ratio Tween20: Poloxamer 188: Phosphatidylcholine = 4.66:1:1, is the most suitable for obtaining NLCs as efficient drug distribution systems.
... NLCs have a core that consists of solid and liquid lipids distributed in aqueous emulsifier solution. The use of NLC ensures the protection of active ingredients from external modifications such as chemical and temperature changes as well as enzymatic activities (Akademia Baru et al. 2015). There are multiple methods available for the preparation of NLC, some techniques that are used include, high-pressure homogenisation, ultrasonication, solvent emulsification evaporative technique, and high shear homogenisation (Jaiswal et al. 2016). ...
The evidence of cannabis exhibiting polypharmacological properties has been accumulating for the past few decades, particularly for its analgesic and anti-inflammatory abilities. However, inconsistent dosage forms and erratic absorption levels prevent medicinal cannabis products from becoming mainstream recommendations for pain management. Current cannabis products fail to address the undesirable characteristics associated with cannabinoids such as low solubility, poor bioavailability, and lack of specificity, all of which contribute to low therapeutic effect. In this narrative view, the pharmacokinetics of cannabis products and possible methods of drug delivery, in the form of carrier systems, will be explored. The incorporation of cannabinoids into carrier systems provides an opportunity to improve absorption levels, increase bioavailability and reduce adverse events allowing for a greater therapeutic effect.
... The pressure made because of sonication assists with defeating the van der Waal's forces of attraction and brings the functional components to the surface of the particles using Hielscher Ultrasound Technology, 2014, which gets captured by the wall material present in the solution. [34] In an ultrasonication technique, properties of treated particles may be changed by using high intensity waves, shear forces, temperature and pressure. [35] On the other hand, lower energy and emulsifier consumption, smaller particle size, lower polydispersity, and greater stability of nano-emulsions are among the key benefits of this technique. ...
Nano-encapsulation in terms of nanotechnology is one of the wide ranged and rapid adopted technologies in food industry. Nanotechnology has modernized the whole food system from production to stored products for the improvement in quality and preservation of nutritional status. Nano-encapsulation is also known as promising technology to protect bioactive components and could be suitable for delivering such protected compounds to target biological systems. In this review, the recent literature highlights the formulation and fabrication of nano-encapsulation using the appropriate wall materials. Moreover, literature also focuses on different methods, which have been used for encapsulation purposes such as coacervation, inclusion complexation, nano-precipitation, emulsification, supercritical fluid technique, ultra-sonification and spray and freeze-drying. Furthermore, this review also discusses the advances in the applications of nano-encapsulation for phenolic compounds, antioxidants, natural food col-orants, antimicrobial agents, essential oils, minerals, flavors and vitamins as nano-carriers in food systems. As reviewed in this study, nanotechnology have ability to improve the food properties either in sensory attributes, storage, target delivery, along with to enhance its nutrition and make it healthier. Nano-encapsulation has played a vital role in approaching the way of advancement of bioactive compounds including their therapeutic potential especially in allied fields, food, and pharmaceutical industry during last decades. ARTICLE HISTORY
... The pressure made because of sonication assists with defeating the van der Waal's forces of attraction and brings the functional components to the surface of the particles using Hielscher Ultrasound Technology, 2014, which gets captured by the wall material present in the solution. [34] In an ultrasonication technique, properties of treated particles may be changed by using high intensity waves, shear forces, temperature and pressure. [35] On the other hand, lower energy and emulsifier consumption, smaller particle size, lower polydispersity, and greater stability of nano-emulsions are among the key benefits of this technique. ...
Nano-encapsulation in terms of nanotechnology is one of the wide ranged and rapid adopted technologies in food industry. Nanotechnology has modernized the whole food system from production to stored products for the improvement in quality and preservation of nutritional status. Nano-encapsulation is also known as promising technology to protect bioactive components and could be suitable for delivering such protected compounds to target biological systems. In this review, the recent literature highlights the formulation and fabrication of nano-encapsulation using the appropriate wall materials. Moreover, literature also focuses on different methods, which have been used for encapsulation purposes such as coacervation, inclusion complexation, nano-precipitation, emulsification, supercritical fluid technique, ultra-sonification and spray and freeze-drying. Furthermore, this review also discusses the advances in the applications of nano-encapsulation for phenolic compounds, antioxidants, natural food colorants, antimicrobial agents, essential oils, minerals, flavors and vitamins as nano-carriers in food systems. As reviewed in this study, nanotechnology have ability to improve the food properties either in sensory attributes, storage, target delivery, along with to enhance its nutrition and make it healthier. Nano-encapsulation has played a vital role in approaching the way of advancement of bioactive compounds including their therapeutic potential especially in allied fields, food, and pharmaceutical industry during last decades.
... Based on the study done by Rosli et al. (2015) and Suhaimi et al. (2017), the size of the particle was depend on the different lipid percentage inside the formulation. The power and time for ultrasonication was fixed throughout the experiment and formulation with 3 % solid lipid and 2 % liquid lipid had effectively reduced the size of the particle. ...
Lemongrass with scientific name Cymbopogon citratrus was widely found in tropical country. The aroma scent released by the lemongrass able to relieve anxiety and rejuvenate us. Lemongrass oil is suitable to use as one of the car freshener ingredient. However, the oil is easily evaporating when expose to high temperature environment. In order to preserve the fragrance release, the objective of this study is to formulate the nanostructured lipid carrier (NLC) encapsulated lemongrass oil using the ultrasonication technique. The characterization of the NLC-Lemongrass were particle size, polydispersity index (PDI), zeta potential, efficiency of the loading and the release rate. The NLC-Lemongrass oil formulation had an average mean particle size of 43.86 nm, PDI of 0.28, zeta potential -42.9 mV and efficiency of the loading 82.13 %, respectively. In addition, after 25 d, the component of the lemongrass oil inside the NLC able to remain at 53.24 %. Therefore, the NLC was successfully encapsulate the lemongrass oil and prolong the aroma release at high temperature environment.
... RLN-NLCs were prepared by an ultrasonication technique as described previously [31]. Briefly, 600 mg of Compritol ® 888 ATO (solid lipid) was melted at 80 • C and 200 mg of Transcutol ® HP (liquid lipid) was added and blended to form a clear lipid phase. ...
Nanotherapeutics in cancer treatment are dominating global science and research, and have been recognized as the pioneering medical care regimen. Raloxifene (RLN) has been used for its anti-proliferative action on mammary tissue, however, it suffers from poor oral bioavailability. This investigation gives an account of the design and development of RLN-loaded nanostructured lipid carriers (RLN-NLCs) using a simple and scalable ultrasonication method for improved oral efficacy and limited offsite toxicity using Compritol® 888 ATO as a solid lipid and Transcutol® HP as a liquid lipid. In addition, the optimized RLN-NLCs were in the nanometric range (121 nm) with high % entrapment efficiency (%EE) (81%) for RLN, and were further freeze-dried in the presence of mannitol to enhance the stability of RLN-NLCs in the dry state for long-term use. Morphological observation under a transmission electron microscope and scanning electron microscope revealed the spherical smooth surface nanometric size of RLN-NLCs. Powder x-ray diffraction confirmed the encapsulation of RLN into the RLN-NLC's matrix with reduced crystallinity of the drug. The in vitro release study showed a burst release for an initial 4 h, and sustained release for up to 24 h. Furthermore, the RLN-NLCs showed higher cytotoxicity towards MCF-7 cells in vitro in comparison to RLN suspension, and an ex vivo intestinal permeation study demonstrated improved intestinal permeability of RLN-NLCs. Moreover, the in vivo pharmacokinetic study in female Wistar rats showed a 4.79-fold increment in oral bioavailability of RLN from RLN-NLCs compared to RLN suspension. Taken together, our results pave the way for a new nanotherapeutic approach towards breast cancer treatment.
... Zeta potential represents the aggregation of the preparation, i.e., a high zeta potential, both negative and positive, indicates a colloidal system that tends to be stable and can prevent particles from aggregating. In general, particles with a zeta potential higher (more positive) than +30 mV or lower (more negative) than -30 mV are considered stable (Rosli et al., 2015). ...
Curcumin is a chemical compound that has low solubility and bioavailability and, for these reasons, limited biological effectiveness. For improvement, the solubility needs to be increased by nanotechnology and nanoparticles, among others. Nanostructured Lipid Carrier (NLC) is a new drug delivery system that offers several advantages, including a significant increase in drug solubility and entrapment efficiency. This study aimed to formulate curcumin into curcumin-loaded NLC preparation and determine its characteristics, absorption efficiency, and drug loading. The formulation used evaporation and solvent diffusion methods with three different concentrations, namely 5%, 10%, and 15%. Spectrophotometry and HPLC were employed to test the absorption efficiency and drug loading capacity. The results showed that the curcumin-loaded NLC preparation containing 10% curcumin had stable characteristics and produced particles sized 17.4 nm with a polydispersity index of 0.574 and zeta potential of -63.43 mV. Based on the spectrophotometry results, the entrapment efficiency was 93.212%, and the drug loading capacity was 0.708%. Meanwhile, the HPLC showed that the entrapment efficiency was 93.007%, and the drug loading capacity was 0.795%.
The anti-oxidant activity and total phenolic content of alcoholic extracts from seven medicinal plants (Asparagus racemosus, Ocimum sanctum, Cassia fistula , Piper betel, Citrus aurantifolia, Catharanthus roseus, Polyalthia longifolia) were evaluated by using a model system consisting of β-carotene, DPPH free radical and Folin-Ciocalteau method. The total Phenolic content of the extracts was determined spectrophotometrically according to the Folin-Ciocalteau procedure and ranged from 366 mg/100g to 212 mg/100g on fresh weight basis. The total flavanoid content of extracts determined by Aluminium chloride colorimetric assay and ranged from 39.84 mg/100g to 15.94 mg/100g of fresh weight. The highest antioxidant activity was demonstrated by Citrus auantifolia (87.05%) followed by Ocimum sanctum (81.80%) and Catharanthus roseus (71.4%). The highest tannin content was found to be in Catharanthus roseus (7.14%) while in case of anthocyanin content the highest value was found to be in Polyalthia longifolia (0.65mg/l). As far as antimicrobial activity is concerned, Ocimum sanctum and Citrus aurantifolia were found to be most potent against Escherichia coli and Staphylococcus aureus whereas Piper betel showed no effect. Except Piper betel all the extracts were able to inhibit the two bacterial strains and the zone of inhibitions ranged from 19.6 mm to 13.5 mm. The minimum inhibitory concentration against E.coli in case of Ocimum sanctum is 10% and against S.aureus it is 20% while in case of Citrus aurantifolia extracts were active even at 10% concentration for E.coli and 15% for S.aureus.
Alopecia is a dermatological disorder, commonly known as hair loss, which affects up to half of the Caucasian male population by middle age, and almost all (95%) Caucasian men by old age. Considering that alopecia affects so many people and that there is currently no scientifically proven treatment with few side effects, new drug-delivery systems able to improve alopecia therapy are urgently required. With this purpose in mind, the present study aimed to develop lipid nanoparticles (nanostructured lipid carriers) with the ability to incorporate and deliver anti-alopecia active compounds (minoxidil and finasteride) into the dermis and hair follicles. Lipid nanoparticles, prepared by ultrasonication method, showed mean particle sizes around 200 nm, which is sufficient for reaching the dermis and hair follicles, and zeta potential values around -30 mV, which indicates good physical stability. Over 28 days of storage, no significant variations in these parameters were observed, which indicates that all nanoformulations are stable in storage over that period. Cryo-scanning electron microscope measurements showed that all the lipid nanoparticles exhibited a spherical shape and a smooth surface regardless of their composition. Differential scanning calorimetry studies allowed the determination of phase transition temperatures and confirmed the recrystallization of the lipid nanoparticles (recrystallization index between 11% and 86%). A high loading efficiency was achieved for finasteride (between 70% and 90%), while less than 30% was achieved for minoxidil nanoparticles, over 28 days. Controlled release assays in physiological conditions demonstrated that nanoparticles loaded with minoxidil yielded a prolonged release, as desired. Penetration assays through pig ear skin demonstrated that nanoparticles loaded with minoxidil and finasteride had low levels of penetration. These results suggest that the proposed novel formulation presents several good characteristics indicating their suitability for dermal delivery of anti-alopecia active compounds.
Purpose
To study the effects of varying lipid concentrations, lipid and oil ratio, and the addition of propylene glycol and lecithin on the long-term physical stability of nanostructured lipid nanocarriers (NLC), skin hydration, and transepidermal water loss.
Methods
The various NLC formulations (A1–A5) were prepared and their particle size, zeta potential, viscosity, and stability were analyzed. The formulations were applied on the forearms of the 20 female volunteers (one forearm of each volunteer was left untreated as a control). The subjects stayed for 30 minutes in a conditioned room with their forearms uncovered to let the skin adapt to the temperature (22°C ± 2°C) and humidity (50% ± 2%) of the room. Skin hydration and skin occlusion were recorded at day one (before treatment) and day seven (after treatment). Three measurements for skin hydration and skin occlusion were performed in each testing area.
Results
NLC formulations with the highest lipid concentration, highest solid lipid concentration, and additional propylene glycol (formulations A1, A2, and A5) showed higher physical stability than other formulations. The addition of propylene glycol into an NLC system helped to reduce the particle size of the NLC and enhanced its long-term physical stability. All the NLC formulations were found to significantly increase skin hydration compared to the untreated controls within 7 days. All NLC formulations exhibited occlusive properties as they reduced the transepidermal water loss within 7 days. This effect was more pronounced with the addition of propylene glycol or lecithin into an NLC formulation, whereby at least 60% reduction in transepidermal water loss was observed.
Conclusion
NLCs with high lipid content, solid lipid content, phospholipid, and lecithin are a highly effective cosmetic delivery system for cosmetic topical applications that are designed to boost skin hydration.
Zerumbone is a natural compound isolated from the fresh rhizomes of Zingiber zerumbet. This bioactive compound has shown a chemo-preventive, anti-inflammatory and free radical scavenging activities. This study examines, the effect of zerumbone on the extent of tissue damage in Cisplatin-induced hepatotoxicity in rats. The rats received a single dose injection of 45 mg kg-1 Cisplatin. Other groups of rats received zerumbone (100 and 200 mg kg-1), corn oil or the vehicle (DMSO) intraperitoneally for 4 days prior to Cisplatin injections. All animals were decapitated 16 h after Cisplatin injection. Trunk blood was collected and analyzed for alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, alkaline phosphatase and gama-glutamyl transferase. Liver tissue was kept for the quantification of malondialdehyde and glutathione levels. Histopathological investigations were carried out and severity of lesions was scored to obtain quantitative data. This study revealed that zerumbone reduced the extent of liver damage and preserved liver functions as proved by microscopic observations and lesion scoring. Increase in liver MDA levels with a simultaneous reduction in GSH in the Cisplatin 45 mg kg-1 group was attenuated by zerumbone treatment (p<0.05). Zerumbone is beneficial in Cisplatin-induced liver dysfunction and organ damage in rats via prevention of lipid peroxidation and preservation of antioxidant glutathione.
Zingiber zerumbet Sm., locally known to the Malay as "Lempoyang," is a perennial herb found in many tropical countries, including Malaysia. The rhizomes of Z. zerumbet, particularly, have been regularly used as food flavouring and appetizer in various Malays' cuisines while the rhizomes extracts have been used in Malay traditional medicine to treat various types of ailments (e.g., inflammatory- and pain-mediated diseases, worm infestation and diarrhea). Research carried out using different in vitro and in vivo assays of biological evaluation support most of these claims. The active pharmacological component of Z. zerumbet rhizomes most widely studied is zerumbone. This paper presents the botany, traditional uses, chemistry, and pharmacology of this medicinal plant.
The objective of the present study was to evaluate the anti-pyretic and analgesic activities of aqueous and ethanol extracts of Zingiber zerumbet rhizomes. The anti-pyretic activity of Zingiber zerumbet (25, 50 and 100 mg kg<SUP>-1</SUP>) was studied in Brewer's yeast-induced pyrexia in rats. The analgesic activity of Zingiber zerumbet (10, 25, 50 and 100 mg kg<SUP>-1</SUP>) was studied using acetic acid-induced writhing in mice. Both aqueous and ethanol extracts of Zingiber zerumbet showed significant anti-pyretic activities in Brewer's yeast-induced pyrexia in rats throughout the observation period of 8 h. The ethanol extract of the rhizomes of Zingiber zerumbet however significantly decreased the writhing movements in mice in acetic acid-induced writhing test. In conclusion, rhizomes Zingiber zerumbet have both analgesic and anti-pyretic activities.
Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) are colloidal carrier systems providing controlled release profiles for many substances. Clotrimazole-loaded SLN and NLC were prepared by the hot high pressure homogenization technique in order to evaluate the physical stability of these particles, as well as the entrapment efficiency of this lipophilic drug and its in vitro release profile. The particle size was analyzed by PCS and LD showing that the particles remained in their colloidal state during 3 months of storage at 4, 20 and 40 degrees C. For all tested formulations the entrapment efficiency was higher than 50%. The obtained results also demonstrate the use of these lipid nanoparticles as modified release formulations for lipophilic drugs over a period of 10 h.
The present study aimed to evaluate influences of mixed lipids and their proportions on formation and properties of nanostructured lipid carriers (NLCs). The physicochemical parameters of drug-free NLCs were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and rheological measurements. In addition, a drug incorporation model was introduced into the NLCs for the application test. The hydrodynamic diameter (Rd) of the final NLCs (varying from 150 nm to 350 nm) was affected by diverse lipids core. DSC results showed that both onset and melting points of NLCs declined due to the addition of the liquid oil, and the liquid oil enabled the melting peak wider, indicating a reduced crystallinity of NLC products which almost coincided with the XRD analysis. Furthermore, rheological studies suggested stronger elasticity property than the viscosity property of the NLC systems. NLCs with high lipids content (20 wt%) had good thixotropy. Conjugated linoleic acid incorporation study showed that the NLC formulation had the well-controlled release profile.
Tamoxifen citrate (Tmx) was formulated in nanostructured lipid carrier system (NLC) using long chain solid lipids(LCSL) and oils(LCO) with the aim to target lymphatic system to improve its bioavailability in plasma and lymphnode (initial sites for metastasis) and reduce its drug associated toxicity. Tamoxifen loaded NLC (Tmx-NLC) was formulated using solvent diffusion technique. Preformulation studies comprised evaluation of drug-excipients compatibility. Solubility of Tmx was screened in LCSL and LCO, surfactants and co-surfactants to identify NLC components. Surfactant co-surfactant combinations were studied for their ability to stabilize the system. Tmx-NLC was physicochemically characterized by TEM, DSC, XRD, and FTIR studies. Drug-excipients chemical compatibility study facilitated anticipation of excipients induced oxidative degradation of Tmx. Suitable storage condition below 30 (o)C could stabilize Tmx. Tmx-NLC with > 90% entrapment efficiency and 215.60 ± 7.98nm particle size were prepared and freeze dried. Freeze dried Tmx-NLC could withstand various gastrointestinal tract (GI) media (pH 1.2, pH 3.5, pH 4.5, pH 6.8, pH 7.4). Dissolution profile of Tmx-NLC in various media showed sustained release pattern irrespective of pH of medium. No significant change in characteristics of Tmx-NLC was observed after 3 months of accelerated stability studies.
Nanostructured lipid carriers (NLC) consisted of solid lipid and liquid lipid are a new type of colloidal drug delivery system, which offer the advantage of improved drug loading capacity and release properties. Surfactants play important roles in the formation and characterization of NLC. In order to investigate the influence of surfactants on properties of NLC, four types of surfactants and their mixtures were used in the absence of model drugs thereby avoiding the interaction between surfactants and drugs. The hot high-pressure homogenization method was employed to produce NLC and the physicochemical properties of NLC, such as particle size distribution, zeta potential and DSC analysis were investigated. The results indicated that ionic surfactants such as sodium deoxycholate (SDC), showed obviously low emulsification efficiency in the preparation. However, it increased the zeta potential of nanoparticles leading to improve the physical stability of the system. Non-ionic emulsifier, especially Poloxamer 188, offered additional steric stabilization effect avoiding aggregation of the nanoparticles in the colloidal system. The formulation in the study combined four types of additives including ionic surfactant (SDC), non-ionic emulsifier (Poloxamer 188 and Tween-80), and Lecithin to obtain favorably stable NLC drug delivery system, which could stabilize for more than 1 year without phase separation at 4 °C.
Itraconazole-loaded NLC for pulmonary application were developed. In Precirol ATO 5 and oleic acid Itraconazole had the highest solubility. The solid lipid and the oil were mixable in a ratio 9:1 possessing a melting point above body temperature. 0.4% Itraconazole was dissolved in this lipid blend. Eumulgin SLM 20 was the stabilizer with the highest affinity to the lipid blend used as particle matrix. 2.5% Eumulgin SLM 20 was sufficient to obtain NLC with a narrow particle size distribution and sufficient stability. The tonicity of the formulation was adjusted with glycerol. Sterility was obtained by autoclaving. Neither the addition of glycerol nor autoclaving had an influence on the particle size and the zeta potential of Itraconazole-loaded NLC. SEM images showed spherical particles confirming the particle size measured by light scattering techniques. An entrapment efficiency of 98.78% was achieved. Burst release of Itraconazole from the developed carrier system was found. Itraconazole-loaded NLC possessed good storage stability. Nebulizing Itraconazole-loaded NLC with a jet stream and an ultrasonic nebulizer had no influence on the particle size and the entrapment efficiency of Itraconazole in the particle matrix, being a precondition for pulmonary application.
The first generation of lipid nanoparticles was introduced as solid lipid nanoparticles (SLN), the second, improved generation as nanostructured lipid carriers (NLC). Identical to the liposomes, the lipid nanoparticles (NLC) appeared as products first on the cosmetic market. The article gives an overview of the cosmetic benefits of lipid nanoparticles, that means enhancement of chemical stability of actives, film formation, controlled occlusion, skin hydration, enhanced skin bioavailability and physical stability of the lipid nanoparticles as topical formulations. NLC are on the market as concentrates to be used as cosmetic excipients, special formulation challenges for these products are discussed. NLC appeared also in a number of finished cosmetic products world-wide. An overview of these products is provided including their special effects due to the lipid nanoparticles, lipids used for their production and incorporated cosmetic actives.
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Curcuminoidsloaded lipid nanoparticles: novel approach towards malaria treatment
- A P Nayak
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- B Madhusudhan
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- A M Manea
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