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Design and preparation lipid polymer hybrid nanocarrier as pulmonary dispersion system using a Novel microwave method
... However, the methods to prepare the LPHNs in these studies were associated with several limitations such as cost, lower stability and time consuming. Recently, a microwave-based method has been used to prepare the LPHNs (11,12) . These reports indicated that the microwave-based method have many merits such as rapid processing, can achieve in both small and large scale, inexpensive, more stable, economical, and absence of impurities (11,12) . ...
... Recently, a microwave-based method has been used to prepare the LPHNs (11,12) . These reports indicated that the microwave-based method have many merits such as rapid processing, can achieve in both small and large scale, inexpensive, more stable, economical, and absence of impurities (11,12) . This research aims to prepare oral felodipine LPHNs to investigate the effect of independent variables which are lipid content, distilled water content, and surface-active agents:cosurfactant blend on the rheological behavior of the nanosystem. ...
... Nine felodipine LPHNs formulations (H1-H9) were prepared using the microwave-based method that was previously described by Drais H K and Hussein A A (11,12) . The hydrophobic mixture was prepared by dissolving chitosan polymer, felodipine, and lauric acid in a blend of cardamom oil and PEG-laurate using a magnetic stirrer device at 1000 rpm for 5 minutes. ...
The rheological behavior among the factors that are present in Stokes law can be used to control the stability of the colloidal dispersion system. Lipid/polymer hybrid nanocarriers (LPHNs) is an interesting colloidal dispersion system that is used for rheological characteristic analysis. The LPHNs are composed of polymeric components and lipids. This research aims to prepare oral felodipine LPHNs to investigate the effect of independent variables which are lipid content, surfactant mixture and distilled water, on the rheological behavior of the nanosystem. A microwave-based technique was successfully used to prepare felodipine LPHNs (H1-H9). The formulations were characterized for particle size and PDI to confirm the colloidal properties of the prepared nanosystem. Therefore, rheological evaluation study of described nanosystems was performed using the coaxial rotational digital rheometer. The outcomes showed that all felodipine LPHNs formulations (H1-H9) had a nanosize and homogenous structure which verified the colloidal features of the nanodispersion systems. The rheogram chart indicated that all felodipine LPHNs formulations (H1-H9) show pseudoplastic flow (non-Newtonian flow), suggesting a shear-thinning property. The microwave-based method successfully produced felodipine LPHNs with excellent physical texture that proves its ability as a nanoparticles preparation technique. The pseudoplastic flow behavior of felodipine LPHNs formulations (H1-H9) suggests that the described nanosystems in this study are physically stable Keywords: Rheology, Felodipine, Lipid-polymer hybrid nanocarriers, Microwave-based method. الصيدلة لكلية التاسع العلمي المؤتمر # ، بغداد جامعة 25-26 اب 2021 * العراق ، بابل ، بابل صحة دائرة ، والبيئة الصحة وزارة. ** ، بغداد ، بغداد جامعة ، الصيدلة كلية ، الصيدالنيات فرع العراق. الخالصة الغروي التشتت نظام استقرار في للتحكم ستوكس قانون في الموجودة العوامل بين الريولوجي السلوك استخدام يمكن. النانوية الناقالت فيلوديبين الشحمي البوليمر من الهجينة (LPHNs) الريولوجية الخصائص لتحليل يستخدم لالهتمام مثير غرواني تشتت نظام هي. تتكون LPHNs ودهون بوليمرية مكونات من. فلوديبين إعداد إلى البحث هذا يهدف LPHNs السلوك على المستقلة المتغيرات تأثير الستقصاء الفم طريق عن النانوي للنظام الريولوجي. فلوديبين لتحضير الميكروويف تقنية استخدام تم (LPHNs H1-H9) بنجاح. التوص عملية في الصيغ جميع تدخل يف و الجسيمات لحجم PDI لتقييم المحوري الدوراني الرقمي االنسياب مقياس استخدام ثم المحضر النانوي للنظام الغروانية الخصائص من للتأكد االنسيابية. فلوديبين تركيبات جميع أن النتائج تظهر (LPHNs H1-H9) ال التشتت لنظام الغروانية السمات تؤكد ومتجانسة نانوية بنية لها نانوي. فلوديبين تركيبات جميع أن إلى البياني الرسم مخطط يشير LPHNs H1-H9)) الكاذب البالستيك تدفق تظهر (النيوتوني غير التدفق) له الذي القص ترقق خاصية. فلوديبين تركيبات بإعداد الميكروويف على المعتمدة الطريقة تقوم LPHNs H1-H9)) ممتا ًا فيزيائي ًا نسيج ُظهر ت التي ، ا زً النانوية الجسيمات لتحضير كأسلوب قدرتها يؤكد وهذا. الفلوديبين تركيبات جميع ُظهر ت (LPHNs H1-H9) يدعم الذي الكاذب البالستيك تدفق النانوي للنظام المادي االستقرار. المفتاحية الكلمات : ، الدهني للبوليمر الهجينة النانوية الناقالت ، الفلوديبين ، الريولوجيا الميكروويف طريقة .
... There are many methods of LPHNs preparation with some limitations such as: the presence of impurities in final products, costly, require high time that delays research field, and low stability. The newly microwave-based method is employed with great success in the formulation of a highly advanced nano system which is LPHNs and characterized by economical, absence of impurities associated with other nanoparticle preparation methods, inexpensive, high stable of final formulation (10)(11)(12) . The single emulsification solvent evaporation technique (SESET) is widely used in the preparation of nanocarriers. ...
... The optimized felodipine LPHNs formulations (HF1-HF3) as shown in Table (1), are immediately used for the study or lyophilized to be filled in hard gelatin capsules. In the lyophilization process (freeze-drying), the samples were first frozen at -20 °C for 2 h, then transferred at -80 o C for 22 h., and then lyophilized at 0.001 mbar at -104 °C for 24 h using lactose 10%(w/w) as a cryoprotectant (10,14) . ...
... The microwave causes dipolar rotation and ionic conduction that cause molecular oscillation and molecular collisions that raise the thermal energy of the system lead to weak bonds disruption. The increased thermal energy for the system create tamed molecules that is more favorable and faster to get self-assembly by the magnetic stirrer agitation to produce felodipine LPHNs formulation (10,14) . The felodipine LPHNs formulations (HF4-HF6) were prepared by single emulsification solvent evaporation technique (SESET) according to specified concentrations of components as shown in Table ( 1). ...
The antihypertensive felodipine is a calcium-channel blocking agent. It is practically insoluble in water and shows low oral bioavailability (15%-20%). This investigation aims to formulate and characterize felodipine lipid polymer hybrid nanocarriers (LPHNs) to be given orally by two nanovesicles formulating methods and make comparative analysis through characterization process and in vitro and ex vivo intestinal permeation evaluation. The felodipine LPHNs formulations (HF1-HF3) were prepared by the new microwave-based method and that felodipine LPHNs formulations (HF4-HF6) were prepared by a single emulsification solvent evaporation technique (SESET). All formulations (HF1-HF6) enter the characterization process. The felodipine LPHNs formulations (HF1-HF6) were prepared successfully and undergo different characterization processes to make a comparative study between formulations prepared by different methods. It was found that formulas prepare by a microwave-based method are most superior to the SESET. The felodipine LPHNs formulations HF1-HF3 has lower particle size, lower PDI and higher zeta potential, significantly higher (p< 0.05) dissolution rate, and significantly higher (p< 0.05) intestinal permeation study than the felodipine LPHNs formulations HF4-HF6. The microwave-based method is a very successful technique in preparing felodipine LPHNs formulations (HF1-HF3) and prepotent to the SESET. All the felodipine LPHNs formulations (HF1-HF6) show extended drug release nanosystem.
... There are many methods of LPHNs preparation with some limitations such as: the presence of impurities in final products, costly, require high time that delays research field, and low stability. The newly microwave-based method is employed with great success in the formulation of a highly advanced nano system which is LPHNs and characterized by economical, absence of impurities associated with other nanoparticle preparation methods, inexpensive, high stable of final formulation (10)(11)(12) . The single emulsification solvent evaporation technique (SESET) is widely used in the preparation of nanocarriers. ...
... The optimized felodipine LPHNs formulations (HF1-HF3) as shown in Table (1), are immediately used for the study or lyophilized to be filled in hard gelatin capsules. In the lyophilization process (freeze-drying), the samples were first frozen at -20 °C for 2 h, then transferred at -80 o C for 22 h., and then lyophilized at 0.001 mbar at -104 °C for 24 h using lactose 10%(w/w) as a cryoprotectant (10,14) . ...
... The microwave causes dipolar rotation and ionic conduction that cause molecular oscillation and molecular collisions that raise the thermal energy of the system lead to weak bonds disruption. The increased thermal energy for the system create tamed molecules that is more favorable and faster to get self-assembly by the magnetic stirrer agitation to produce felodipine LPHNs formulation (10,14) . The felodipine LPHNs formulations (HF4-HF6) were prepared by single emulsification solvent evaporation technique (SESET) according to specified concentrations of components as shown in Table ( 1). ...
... However, the methods to prepare the LPHNs in these studies were associated with several limitations such as cost, lower stability and time consuming. Recently, a microwave-based method has been used to prepare the LPHNs (11,12) . These reports indicated that the microwave-based method have many merits such as rapid processing, can achieve in both small and large scale, inexpensive, more stable, economical, and absence of impurities (11,12) . ...
... Recently, a microwave-based method has been used to prepare the LPHNs (11,12) . These reports indicated that the microwave-based method have many merits such as rapid processing, can achieve in both small and large scale, inexpensive, more stable, economical, and absence of impurities (11,12) . This research aims to prepare oral felodipine LPHNs to investigate the effect of independent variables which are lipid content, distilled water content, and surface-active agents:cosurfactant blend on the rheological behavior of the nanosystem. ...
... Nine felodipine LPHNs formulations (H1-H9) were prepared using the microwave-based method that was previously described by Drais H K and Hussein A A (11,12) . The hydrophobic mixture was prepared by dissolving chitosan polymer, felodipine, and lauric acid in a blend of cardamom oil and PEG-laurate using a magnetic stirrer device at 1000 rpm for 5 minutes. ...
The rheological behavior among factors that are present in Stokes law can be used to control the stability of the colloidal dispersion system. The felodipine lipid polymer hybrid nanocarriers (LPHNs) is an interesting colloidal dispersion system that is used for rheological characteristic analysis. The LPHNs compose of polymeric components and lipids. This research aims to prepare oral felodipine LPHNs to investigate the effect of independent variables on the rheological behavior of the nanosystem. The microwave-based technique was used to prepare felodipine LPHNs (H1-H9) successfully. All the formulations enter the characterization process for particle size and PDI to ascertain the colloidal properties of the prepared nanosystem then use coaxial rotational digital rheometer for rheological evaluation. The outcomes show that all felodipine LPHNs formulations (H1-H9) had a nanosize and homogenous structure that ascertain colloidal features of the nanodispersion system. The rheogram chart indicates that all of the felodipine LPHNs formulations (H1-H9) show pseudoplastic flow (non-Newtonian flow) that have shear-thinning property. The microwave-based method prepares felodipine LPHNs formulations (H1-H9) that show excellent physical texture that ascertains its ability as a technique for the preparation of nanoparticles. All of the felodipine LPHNs formulations (H1-H9) show pseudoplastic flow that supports the physical stability of the nanosystem.
... The microwaves have three main attributes that facilitate them to be employed in pharmaceutical research and industry which are-reflection by metal substances, it is absorbed by pharmaceutical materials, and able to pass through the plastic, glass, paper, and similar ingredients. [13][14][15][16][17][18] This research aims to prepare and characterize oral felodipine LPHNs to increase solubility and control felodipine delivery to improve bioavailability and enhance patient compliance. ...
... The remaining of water molecules were removed by secondary drying process at 40ºC and 0.1 mbar for 2 hours, using lactose 10% (w/w) as cryoprotectant. [13][14][15][16][17][18] Evaluation of physical stability of felodipine LPHNs formulations using thermodynamic stability measurements The thermodynamic stability studies were achieved by the following tests. 13,19 Centrifugation assay The felodipine LPHNs formulations were centrifuged at the 5000 rpm for 30 minutes and checked physical stability parameters of nanovesicles. ...
... [13][14][15][16][17][18] Evaluation of physical stability of felodipine LPHNs formulations using thermodynamic stability measurements The thermodynamic stability studies were achieved by the following tests. 13,19 Centrifugation assay The felodipine LPHNs formulations were centrifuged at the 5000 rpm for 30 minutes and checked physical stability parameters of nanovesicles. ...
Purpose: Felodipine, is a calcium-channel antagonist used for hypertension and angina pectoris. It is practically insoluble in aqueous media and shows low oral bioavailability (15%-20%). This investigation aims to prepare and characterize oral felodipine lipid-polymer hybrid nanocarriers (LPHNs) to increase solubility and control delivery for increasing bioavailability and enhance patient compliance.
Methods: The newly microwave-based method was prepared with felodipine LPHNs (H1-H35) successfully. The (H1-H35) were subjected to thermodynamic stability experiments. After that, select nine felodipine LPHNs (F1-F9) that have smart physical stability for further optimization of different characterization processes.
Results: The felodipine LPHNs (F4) are considered the most optimized formula. It was characterized by lower particle size (33.3 nm), lower PDI (0.314), high zeta potential (13.6 mV), entrapment efficiency is (81.645% w/w), drug loading is (16.329% w/w), the pH value is 4, excellent percent of light transmittance (95.5%), pseudoplastic rheogram, significantly high (P < 0.05) dissolution rate with sustained drug delivery and success ex-vivo intestinal permeation attributes. The (F4) subject for further investigations of Fourier transformed infrared spectroscopy (FTIR), atomic force microscopy (AFM), and transmission electron microscopy (TEM). The results of FTIR, AFM, and TEM indicate there is no interaction between the felodipine and excipients and that the particulate system in the nanoscale dispersion system confirms the high stability.
Conclusion: The optimized felodipine LPHNs (F1-F9) formulations were smart formulations for sustained oral delivery of felodipine and that F4 was the most optimized formula according to its characterization processes.
... It was merged the properties of both polymeric nanocarriers and liposome as lipid base nanoparticles. The LPHNs was contained three components which are lipid part, polymer constituent and outer surface active agent layer, which act as a stealth coating that prolongs time duration of nanocarriers in vivo circulation as well as providing steric stabilization during long term storge [16][17][18] . In contrast to other carriers, the LPHNs were shown important features, including the structural components diversification,ability to encapsulate the hydrophilic and hydrophobic therapeutic moieties, provide greater controlled drug release, ability to higher encapsulation biocompatibility, improve solubility and permeability of bioactive agents, improved in vitro and in vivo stability and provie easy cellular uptake [17][18][19] . ...
... The LPHNs was contained three components which are lipid part, polymer constituent and outer surface active agent layer, which act as a stealth coating that prolongs time duration of nanocarriers in vivo circulation as well as providing steric stabilization during long term storge [16][17][18] . In contrast to other carriers, the LPHNs were shown important features, including the structural components diversification,ability to encapsulate the hydrophilic and hydrophobic therapeutic moieties, provide greater controlled drug release, ability to higher encapsulation biocompatibility, improve solubility and permeability of bioactive agents, improved in vitro and in vivo stability and provie easy cellular uptake [17][18][19] . The aim of this research to study permeability coefficient for NE, NLCs and LPHNs based nanogel through biological membrane using carvedilol as bioactive agent. ...
Carvedilol was antihypertensive and antioxidant properties. It was practically water insoluble. It undergoes extensive hepatic first pass metabolism. The aim of this research to study permeability coefficient for NE, NLCs and LPHNs based nanogel through biological membrane using carvedilol as transdermal drug delivery system (TDDS). Aqueous phase titration, ultrasonic emulsion evaporation and microwave-based methods were used to prepare NE1-NE3, NLC1-NLC3 and LPHN1-LPHN3 respectively then subject to various measurements. The formulated lipid-based nanoparticles NE1-LPHN3 were employed as base to prepare lipid base nanogel G1-G9 that was compare to already prepared conventional gel of carvedilol (G). It was found colloidal features associated with the carvedilol loaded lipid-based nanoparticles NE1-LPHN3. The biomembrane permeation evaluation of G1-G9 formulations was indicated that the permeability coefficient (cm/min) of drug was significantly higher (p-value <0.05) for G1 and was significantly lower (p-value < 0.05) for conventional carvedilol gel (G). The preparation and evaluation processes were emphasized that G1-G9 suitable to deliver across biomembrane. The drug that was contained in LPHN based nanoglobules had lower ability to pass through experimental skin that gave it more ability to control drug diffusion in comparison to NE and NLCs.
... give combined features of polymeric nanocarriers and lipid-based nanocarriers [11][12][13]. The lipid enhances solubility and increases entrapment efficiency of hydrophobic drugs, ...
The prednisolone was very slightly soluble in water. It was a curative agent against oral recurrent aphthous stomatitis. The main objective of this study is to design, prepare, and evaluate a hybrid nanogel of prednisolone as a topical dosage form to increase prednisolone solubility, stability, and therapeutic activity. The microwave-based method prepared nine prednisolone lipid polymer hybrid nanocarriers LPHNs formulations (H1-H9). The conventional prednisolone gel (G) was prepared by solvent diffusion. The H1-H9 was evaluated thermodynamically and entered into characterization processes. The hybrid nanogels HN1-HN9 formulations were tested for various evaluations. All the H1-H9 formulations showed high thermodynamic stability and nanosized globules, low polydispersity index, acceptable surface charge, entrapment efficiency, and drug loading. The evaluation processes indicate stable organoleptic properties, high homogeneity, fair pH and spreadability coefficient values with plastic viscosity and no erythemic reaction. The profile of prednisolone release and permeability coefficient (cm/min) was significantly higher (p-value <0.05) for HN3 and significantly lower (p-value < 0.05) for conventional prednisolone gel (G). The optimized HN1-HN9 formulations were promised drug delivery systems for treating recurrent aphthous stomatitis and a wide variety of oral lesions in addition to local and transdermal delivery of various therapeutic agents and cosmetics.
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