Table 6 - uploaded by May Almukainzi
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This literature review is a compilation of the composition and, in most cases, the preparation instructions for simulated biological fluids that may be used as dissolution media in the evaluation of dissolution profiles and amount of drug released from pharmaceutical dosage forms. The use of simulated biological fluids can give a better understandi...
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Context 1
... recent data in humans indicate that the pH in the upper small intestine decreases rather slowly after meal intake (Table 6) (13,14). ...
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Curcumin is a natural active principle with antioxidant, antibacterial and anti-inflammatory properties. Its use is limited by a low water solubility and fast degradation rate, which hinder its bioavailability. To overcome this problem, curcumin can be delivered through a carrier, which protects the drug molecule and enhances its pharmacological ef...
Citations
... The solubility study of pure DRVE in simulated vaginal fluid and water at various pH conditions was performed. pH of the prepared Simulated Vaginal Fluid (SVF) (Marques et al., 2011) was adjusted by using 0.2M NaOH and 0.2M HCL. An excess amount of pure drug was added to 10 mL simulated vaginal fluid of pH ranging from 1.5, 2.5, 3.5, 4.5, 5.5, 6.5 to 7.5 and was taken into a conical flask. ...
... The bioaccessible fraction of metals contained in PM is often assessed through experiments in which samples are solubilised in surrogate lung fluids with various degrees of complexity (Marques et al. 2011;Wiseman 2015;Coufalík et al. 2016;Innes et al. 2021). The most used surrogate lung fluid is the Gamble's solution (Berlinger et al. 2008;Colombo et al. 2008;Coufalík et al. 2016;Huang et al. 2016Huang et al. , 2018Kumar et al. 2017;Pelfrêne et al. 2017;Hernández-Pellón et al. 2018;Wiseman et al. 2018;Xie et al. 2019). ...
Environmental context. Metals in airborne particles can interact with lung fluids once particles are inhaled. Water solubility of particle-bound metals is often used to define their bioavailability. We show that particle-bound metals exhibit a complex dissolution kinetics in a surrogate lung fluid, their solubility and dissolution kinetics are driven by the fluid composition, and only to a minor extent by atmospheric aqueous phase processing of aerosols. ABSTRACT Rationale. Metals in airborne particles can interact with lung fluids once particles are inhaled and cause oxidative stress. Their oxidative potential is dependent on their solubility and dissolution kinetics in the lung fluids. Methodology. In this study, we collected PM 2.5 samples from the city of Padova (Italy), in the northern Italian Po Valley. We investigated the solubility and dissolution kinetics of particle-bound metals in a surrogate epithelial lining fluid (SELF) and compared the results to those obtained for a fog water. Results. We found that most elements present a complex dissolution kinetics characterised by three phases: (1) immediate dissolution, (2) first-order dissolution, and (3) first-order precipitation. We observed that the speciation of metal ions in the SELF influences the dissolution kinetics of each element. We also found that atmospheric aqueous phase processing in fog can influence the dissolution kinetics of the elements in SELF. Discussion. The speciation study showed that the SELF composition is the main driver of metal solubility and dissolution kinetics with only a minor influence of atmospheric fog processing. Therefore, metal bioavailability is mainly determined by the biological fluid composition.
... The pH of the prepared hydrogels (Table 1) was within the range of 5.64-6.25, which corresponds to the physiological pH of the oral cavity [24]. According to the calculated entrapment efficiency (%EE) values (Table 2), the ATC loading corresponded to the theoretical drug content within the hydrogels and lyophilizates. ...
... The implemented modifications of the SSS, either by enriching it with PEG 400/Tween 80-solubilizer and surface active agents, respectively-or acidifying it, were fruitless since these modifications interfered with the HPLC data collection. With regard to acidifying the medium, our previous research pointed to a significant impact of pH change (to reflect the oral cavity conditions before and after a meal [24]) on CH dissolution and the subsequent disruption of CH PECs [25], but that impact was not observed here. As the tested solubility of ATC in acetonitrile was as low as for the aqueous solutions, disrupting the PEC particles using the mixture of acetonitrile and a potassium dihydrogen phosphate buffer (pH 3.0) was considered key for successful ATC liberation. ...
... The implemented modifications of the SSS, either by enriching it with P 400/Tween 80-solubilizer and surface active agents, respectively-or acidifying it, w fruitless since these modifications interfered with the HPLC data collection. With reg to acidifying the medium, our previous research pointed to a significant impact of change (to reflect the oral cavity conditions before and after a meal [24]) on CH dissolut and the subsequent disruption of CH PECs [25], but that impact was not observed h As the tested solubility of ATC in acetonitrile was as low as for the aqueous solutio disrupting the PEC particles using the mixture of acetonitrile and a potassium dihydro phosphate buffer (pH 3.0) was considered key for successful ATC liberation. Furthermo in addition to the low pH of the phosphate buffer, the impact of its ionic strength on stability of drug-polymer or polymer-polymer bonds must be noted [13]. ...
Atorvastatin calcium, an antifungal agent, has the potential to be repositioned/repurposed to combat the increasing antimicrobial resistance. However, one of the most crucial issues in developing atorvastatin calcium-loaded products with a topical antifungal effect is achieving the optimal release and dissolution rates of this statin to produce the desired therapeutic effect. In this paper, we report on the development and pharmaceutical assessment of hydrogels composed of low-molecular-weight chitosan, tragacanth, and xanthan gum/pectin/κ-carrageenan as potential drug carriers for atorvastatin calcium for buccal delivery. Multidirectional analysis of the carriers with regard to their drug-release profiles and mucoadhesive, antimicrobial, and cytotoxic properties was accompanied by an evaluation of the freeze-drying process used to improve the hydrogels’ applicability. Using differential scanning calorimetry, Fourier transform infrared spectroscopy, and scanning electron microscopy techniques, the role of lyophilization in enhancing atorvastatin calcium delivery from polyelectrolyte complex-based matrices via drug amorphization was demonstrated. The freeze-dried hydrogels had significantly improved release and dissolution rates for the amorphic statin. Therefore, there is great potential for the use of lyophilization in the design of polyelectrolyte complex-based semi-solids in usable dosage forms for numerous crystalline and poorly water-soluble active substances.
... The surface charge of the nanoparticles obtained and, thus, the stability was measured via laser Doppler micro-electrophoresis at 25 • C after adding them to simulated body fluid (SBF), pH 7.25. The SBF was prepared using the method presented by Marques et al. [28]. Simulated body fluid was chosen because it has ion concentrations nearly equal to those of human plasma. ...
... The drug loading and release capacity of polymer nanoparticles depends on their behavior in the aqueous environment, more precisely on their ability to swell and allow drug molecules to penetrate through the polymer network. To determine the swelling capacity of the obtained nanoparticles, a buffer solution was used that has ion concentrations nearly equal to those of human plasma (simulated body fluid-SBF with pH 7.25) [28]. ...
Background/Objectives: Even with improvements in surgical techniques and the application of appropriate antibiotic prophylaxis, wound infections are still major public health problems in low- and middle-income countries. This study proposes the design of new particulate polymeric matrices based on chitosan (CS) for the controlled release of Metronidazole (MTZ), in order for it to be used for the treatment of Clostridium perfringens infections. Methods: The nanoparticles were prepared via inverse emulsion using tannic acid (TA) and sodium tripolyphosphate (TPP) as cross-linking agents. The ratio of CS to TPP, the concentration of CS solution, and the ratio of CS to TA were varied to optimize the synthesis procedure. Nanoparticles have been characterized based on several points of view in order to correctly correlate their properties with synthesis parameters. Results: The FTIR spectra of the analyzed nanoparticles confirmed both the formation of hydrogen bonds between CS and TA and the ionic cross-linking of CS with TPP. The average diameters of the nanoparticles ranged from 70 to 170 nm, whereas the zeta potential values were around 8 mV. Their swelling degree in a weak basic environment, as well as the drug loading/release capacity was influenced, as expected, by the synthesis parameters. The obtained nanoparticles were tested in vitro to evaluate their behavior in the blood environment, the cytotoxic effect, and the antimicrobial activity of nanoparticles loaded with MTZ against Clostridium perfringens cultures. Conclusions: The in vitro obtained results demonstrate that these non-hemolytic and non-cytotoxic particles can be efficient drug delivery systems for the treatment of Clostridium perfringens in wound infections.
... A sample of the mat (10 mg) was placed in a dissolution medium (2.5 mL) and then incubated at 37 • C. The dissolution medium used was a salivary fluid simulator (SFS with pH 6.8) prepared by dissolving 8.00 g sodium chloride, 0.19 g monobasic potassium phosphate, and 2.38 g dibasic sodium phosphate in 1 L distilled water; if necessary, the pH of the resulting solution was adjusted to 6.8 [40]. At certain time intervals, 2 mL of the medium was withdrawn for CP quantification; the dissolution medium was replenished with fresh SFS. ...
The application of electrospinning technologies for the preparation of mats based on mucoadhesive polysaccharides, such as chitosan (CS), is an attractive strategy for the development of biopolymeric delivery systems for topical corticosteroids. In this work, an electrospinning technique is described for the preparation of CS-based mats doped with halloysite nanotubes (HNTs) with modified release of clobetasol propionate (CP). The optimized composition of the electrospinning solution was determined: 2.4% solution of CS in 46% acetic acid with addition of PEO (10% of CS mass) and HNTs (5% of CS mass); CP was introduced as an ethanol solution at the rate of 2 mg CP per 1 g of the obtained nonwoven material. The process parameters (the electrospinning voltage of 50–65 kV, the rotation speed of the spinning electrode of 10 min⁻¹, and the distance between the electrodes of 24 cm) were also optimized. The developed technology allowed us to obtain homogeneous nanofiber mats with excellent mechanical properties and biphasic drug release patterns (66% of CP released within 0.5 h and 88% of CP released within 6 h). The obtained nanofiber mats maintained the anti-inflammatory activity of corticosteroid at the level of free CP and showed no cytotoxicity.
... The simplest simulated gastric fluids are only adjusted by hydrochloric acid, but some contain sodium, gastric pepsin, and mucin [45,70]. Likewise, intestinal conditions are also simulated by combining simulated intestinal fluids, where the pH is adjusted to 6.5-7.0 and may contain additional components such as bile and pancreatic enzymes [51,70]. These in vitro static models have been widely adopted to Content courtesy of Springer Nature, terms of use apply. ...
The field of probiotics has garnered significant attention due to their potential health benefits, such as enhancing gut health and immune response. The effective delivery of probiotics through microencapsulation is crucial due to the sensitivity of probiotics to environmental stresses. Mathematical modeling offers profound insights into the growth, survival, inactivation, and release dynamics of microencapsulated probiotics, providing a basis for optimizing formulation and predicting behavior under various conditions. Although some of these subjects are cross-sectionally imported from the field of drug delivery, there are no specific papers that comprehensively discuss the mathematical modeling of probiotic microencapsulation from production to delivery. Thus, this paper aims to review the current landscape of mathematical models utilized in the microencapsulation of probiotics in different timelines, including cell culturing, microencapsulation process, storage, and delivery in the gastrointestinal tracts. Predictive microbial models, empirical reaction models, and drug release models were highlighted in each activity. In addition to the principles and equations, recent studies on the application of kinetic models for probiotics and their microcapsules were summarized and discussed. The review emphasizes the necessity of a mathematical approach for the comprehensive understanding of microencapsulated probiotics, combined with insights into food chemistry, microbiology, and engineering, to innovate and advance the application of probiotics for health improvement.
... CP-PLGA NPs were suspended in triplicate in either PBS (pH 7.4) or simulated lung fluid/Gamble's Solution. 48 These suspensions were allowed to shake at 37°C over a period of 7 days, with DLS and ZP measurements being collected daily. ...
Idiopathic pulmonary fibrosis (IPF) is a chronic interstitial disorder of the respiratory system that can be debilitating as it progresses and has experienced a slow rise in incidence in past...
... The dissolution profiles of micronized FP/SX/TB-loaded DPI were assessed using a USP dissolution tester equipped with a paddle agitator (PTWS-1220; Pharma test apparatus AG, Darmstadt, Germany). The filter holder was placed in a dissolution vessel, and 500 mL of simulated lung fluid was used as dissolution media [19]. The dissolution media was maintained at a temperature of 37 ± 0.5 • C with an agitation speed of 75 rpm. ...
Background/Objectives: Inhaler devices have been developed for the effective delivery of inhaled medications used in the treatment of pulmonary diseases. However, differing operating procedures across the devices can lead to user errors and reduce treatment efficacy, especially when patients use multiple devices simultaneously. To address this, we developed a novel dry powder inhaler (DPI), combining fluticasone propionate (FP), salmeterol xinafoate (SX), and tiotropium bromide (TB) into a single device designed for bioequivalent delivery compared to existing commercial products in an animal model. Methods: The micronized FP/SX/TB-loaded capsule was prepared by sieving, blending, and filling capsules. Capsule suitability of the drugs was investigated from the comparison of the stability of drugs within various capsule formulations to that of commercial products. The particle size of the drugs was adjusted using spiral air jet milling, and the ratio of lactose hydrate carriers was optimized by comparing the aerodynamic particle size distribution (APSD) with that of commercial products. To investigate the bioequivalence of micronized FP/SX/TB-loaded DPI to commercial products, the dissolution profile of FP/SX/TB particles and pharmacokinetics in rats were evaluated and compared to commercial products. Results: Capsules with hydroxypropyl methylcellulose (HPMC) without a gelling agent showed superior stability of the drugs compared to commercial products. The deposition pattern was influenced by the particle size of the drugs, and fine particle mass exhibited a significant correlation with the amount of fine carrier. Micronized FP/SX/TB-loaded DPI gave a similar APSD and dissolution profile compared to the commercial products and showed dose uniformity by the DPI device. Furthermore, micronized FP/SX/TB-loaded DPI exhibited bioequivalence to commercial products, as evidenced by no significant differences in pharmacokinetic parameters following intratracheal administration in rats. Conclusions: A novel triple-combination DPI containing FP/SX/TB was successfully developed, demonstrating comparable pharmacological performance to commercial products. Optimized FP/SX/TB-loaded DPI with HPMC capsule achieved bioequivalence in rat studies, suggesting its potential for improved patient compliance and therapeutic outcomes. This novel single-device DPI offers a promising alternative for triple therapy in pulmonary diseases.
... Polysorbate 80 and Triton X-100 were purchased from Sigma Aldrich (Darmstadt, Germany), and HPLC-grade methanol was purchased from E. Merck (Darmstadt, Germany). The simulated saliva fluid (SSF, pH 4.6) composed of 0.1 M disodium hydrogen phosphate and 0.1 M potassium dihydrogen phosphate was prepared according to (Marques et al., 2011). A reference drug, Latuda tablets containing an 18.5 mg dose of Lur (lot 0018, expiration date 03/2027), was from Angelini, Rome, Italy. ...
... Dissolution/release studies were carried out for 24 h in Simulated Lung Fluid 4 (SLF, pH 7.4, DPPC 0.2% (w/v)) [49]. For the microparticles, 5 mg of each sample was dispersed in a dialysis tube, Pur-a-Lyzer (regenerated cellulose membrane, MWCO 3.5 KDa), with 800 µL of SLF. ...
Background/Objectives: Curcumin is well known for its great anti-inflammatory and antioxidant efficacy, representing a potential strategy for the treatment of respiratory disorders. However, several drawbacks, such as chemical instability, poor water solubility and rapid metabolism, result in low bioavailability, limiting its clinical applications. In this study, curcumin nanocrystals were incorporated into mannitol-based microparticles to obtain an inhalable dry powder. Methods: A curcumin nanosuspension was produced by wet-ball media milling and thoroughly characterized. Spray drying was then used to produce mannitol microparticles incorporating curcumin nanocrystals. In vitro release/dissolution tests were carried out in simulated lung fluids, and the aerosolization properties were evaluated using a Next-Generation Impactor (NGI, Apparatus E Ph. Eu.). Results: The incorporation of curcumin nanocrystals into mannitol-based microparticles influenced their morphological properties, such as geometric diameters, and flowability. Despite these changes, nebulization studies confirmed optimal MMAD values (<5 µm), while multi-step dissolution/release studies evidenced the influence of mannitol. Conclusions: The developed curcumin nanocrystals-loaded mannitol microparticles show promise as an inhalable treatment for respiratory diseases, combining effective aerodynamic properties with controlled drug release.
