Solvent Diffusion Technique Research Articles

Optimization, Formulation, and Ex vivo Evaluation of Solid Lipid Nanoparticles for Transdermal Delivery of Diltiazem Hydrochloride.

Cardiac arrhythmia, is a medical condition that reduces the heart's efficiency in pumping blood, and can be fatal, requires long-term management with conventional drugs, despite their limited efficacy. Diltiazem hydrochloride, chosen as a model drug, has a short biological half-life and extensive metabolism. Administering drug through skin is challenging, particularly due to the penetration via stratum corneum. However, solid lipid nanoparticles as a particulate carrier system can enhance its permeation and bioavailability. The study aimed to develop a matrix type transdermal patch with diltiazem hydrochloride encapsulated in solid lipid nanoparticles Methods: The study used the solvent diffusion technique to prepare SLNs by mixing the drug and solid lipid in an organic phase at 80°C, then slowly adding it to an aqueous phase with continuous stirring for 45 minutes. The resulting nanodispersion was freeze-dried and analyzed for morphological studies, encapsulation efficiency & drug content. A patch was formulated using solvent evaporation technique, incorporating HPMC E50 (2% w/v), propylene glycol, and ethanolic oleic acid (1.5% v/v). SLNs loaded with diltiazem hydrochloride taken equivalent to diltiazem hydrochloride dose in the transdermal patch. The patch was then evaluated for In vitro and skin permeation studies. The result showed a positive correlation between lipid concentration and particle size. Probe sonication and homogenization increased particle size, while stirring speed reduced it. SEM and TEM images confirmed spherical particles with a size of 488.1±4.01nm and an entrapment efficiency of 55.03±1.99%. Drug release studies demonstrated 70.7% drug release from lipid matrix over 24 hrs. The formulated patch with uniform SLN distribution, had a drug content 89.37 ± 0.04% with a surface pH of 6.1 ± 0.53, close to skin pH. The uniformity of content in 3x3 patch estimated to be 14.587 ± 1.404 mg, close to the theoretical content 16.318 ± 1.08 mg, confirmed homogenous distribution of diltiazem hydrochloride SLNs throughout the patch diameter. Cumulative amount released from patch formulation at pH 5.6 and pH 7.4 was 518.1414μg/cm2 and 404.4466 μg/cm2. Synergistic flux enhancement was observed with oleic acid propylene glycol blend. Ex vivo study of the patch showed steady-state flux of 6.9 μg/cm2/hr, permeability coefficient 0.00362 cm/hr, diffusion coefficient 0.000103 cm/hr, cumulative drug permeation (Dmax) 814.885 μg after 24 hrs, and followed a Higuchi-matrix release model. The developed patch possessed improved bioavailability with reduced dosing and enhanced patient compliance.

A novel strategy to produce spherical SBA-15 by polymeric macrospheres as a template for drug delivery

AbstractMesoporous silica SBA-15 has been a material widely studied for drug delivery due to its high biocompatibility and chemical stability, its ordered mesoporous cavities allow drug loading. However, it has a non-spherical particle shape, making it difficult to use in solid dosage forms, where spherical particles are preferred for better flow and distribution. In this regard, this study presented a novel strategy to produce spheric SBA-15 using polymeric macrospheres of a pharmaceutical grade acidic-resistant copolymer (Eudragit®S) stabilized with Pluronic® 123, as a template. The macrospheres of Eudragit®S were fabricated using the double emulsion (W1/O/W2) solvent-diffusion technique and then were used as a template to synthesize macrospheres of SBA-15 following acidic hydrolysis. The physicochemical analysis revealed that the SBA-15 has a spherical morphology (SEM) with pores arranged in a hexagonal lattice (TEM). The XRD showed signals at 0.71, 0.88 y 2.03 °2θ, that were indexed at the Miller indices (100), (110), (200). Nitrogen adsorption-desorption isotherms (type IV, H3) demonstrated mesoporous characteristics with a pore size of 9.3 nm, a wall thickness of 3 nm, a pore volume of 0.7538 cm³g−1, and a surface area of 640 m²g−1. These SBA-15 macrospheres also showed a zero-order release of ibuprofen. The SBA-15 formation using Eudragit®S macrospheres suggests that P123 on the macrosphere acts as a spherical core, as shown by FT-IR analysis. The acid-resistant copolymer maintained macrosphere integrity, enabling the assembly of the SBA-15 mesostructure in a 24-hour manufacturing time under acidic conditions.

Formulation and Evaluation of Nicotinamide Microsponges – The First Step Towards the Development of a Novel Topical Dosage Form

The objective of this work was to formulate and analyze microsponges of nicotinamide. The said formulation was created using the emulsion solvent diffusion technique, and a 3 level two factor-based factorial design was applied to optimize the effect of the stabilizer (X1), as well as drug (X2), amounts on the entrapment efficiency (Y1) and average particle size (Y2). Various parameters, such as flow characteristics, percentage yield, drug concentration, in-vitro drug release tests, entrapment efficiency, and scanning electron microscopy (SEM), were evaluated. All parameters were found to be within the acceptable range. Design Expert 13 was employed to optimize the microsponges, and the optimal batch was determined by examining the desirability data. From this analysis, the optimal amounts of drug and stabilizer were found to be 302.87 and 59.71 mg, respectively. The reliability of the preparation and evaluation of the optimized batch was confirmed by a less than 5% discrepancy between the observed and predicted values of parameters. SEM images revealed that the microsponges were prepared with uniform and spherical morphology. The study concluded that nicotinamide microsponges were successfully prepared and evaluated. Further steps will involve incorporating this formulation into a novel topical dosage form.

Evaluating the potential of ethyl cellulose/eudragit-based griseofulvin loaded nanosponge matrix for topical antifungal drug delivery in a sustained release pattern

Fungal infections are very alarming nowadays and are common throughout the world. Severe fungal infections may lead to a significant risk of mortality and morbidity worldwide. Sustained delivery of antifungal agents is needed to mitigate this problem. In the current study, an attempt has been made to formulate griseofulvin-loaded nanosponges using the quasi-emulsion solvent diffusion technique. For characterization, griseofulvin loaded nanosponges were tested by different instrumental techniques such as optical microscopy, scanning electron microscopy (SEM), powder X-ray diffractometer (PXRD), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and transmission electron microscopy (TEM). The antifungal activity of the nanosponges was assessed against Candida albican strain using the agar well-diffusion method. Finally, the drug-loaded nanosponges' in vitro sustained release activity was evaluated. FTIR spectra showed no chemical interference between the drug and polymers. Some of the peaks of the drug are not visible in the FTIR spectrum, which suggests drug entrapment. PXRD data showed that the drug lost its high crystallinity when entrapped in the nanosponge matrix. From the morphological studies via SEM and TEM, a brief idea of the surface morphology of the nanosponges was obtained. The small pores throughout the structure proved its high porosity. The antifungal sensitivity assay was successful, and a zone of inhibition was observed in all the formulations. The in-vitro drug release study showed sustained behaviour. The sustaining effect was due to the polymer and cross-linker used, which gave rise to a porous scaffold matrix. From the results, it can be concluded that griseofulvin-loaded nanosponges can be used for antifungal drug delivery against various topical skin infections.

MICROBALLOONS: A PROMISING APPROACH FOR GASTRORETENTIVE DRUG DELIVERY SYSTEM AND THEIR ADVANTAGES, LIMITATIONS, RECENT ADVANCEMENT IN DRUG DELIVERY SYSTEM, PATENTS AND FUTURE ASPECTS

The key objective of the present review was to collect the latest literature on technological advancements towards microballoons as novelistic buoyant drug delivery systems. Microballoons are hollow microspheres with a potential approach for gastric retention, offering controlled release of the drugs. It offers prominent targeting of drugs in the stomach. More significantly, it is an anticipated drug delivery system in the gastrointestinal tract’s upper section. At a high pH environment, this drug delivery system improves the solubility of less soluble drugs. It is an innovative and authenticated drug delivery system, specifically for those drugs which are unable to tolerate the acidic pH. The microballoons are developed by several techniques like Solvent Evaporation, Solvent Diffusion-Evaporation, Solvent Diffusion and Spray Drying techniques, to develop the space of empty inner core. Moreover, this manuscript covers significance, limitations, applications, list of polymers used, characterization, formulation design and evaluation parameters of microballoons.

Formulation and Evaluation of Miconazole Nanocapsules

Using the emulsion solvent diffusion technique, the current study's goal was to create and analyze miconazole nanocapsules. Ethyl cellulose as well as HPMC nanocapsules were used to fill the miconazole, which has been produced using the emulsion solvent diffusion method. The FTIR data showed that the miconazole nanocapsules filled with ethyl cellulose nanocapsules were stable and that there was no drug-polymer interaction. To determine whether there is no incompatibility in the formulation, compatibility investigations like FTIR & DSC were utilized. The morphological particle size of miconazole nanocapsules is assessed using SEM. This complete formulation codes for the nanocapsules were F1 to F8. The optimum formulation F6's in vitro dissolution rate was found to be 75.22 percent. A variety of mathematical models, including the zero order, first order, Higuchi matrix, and Korsmeyer peppas model, were fitted to the data on drug dissolution in vitro. The model that the miconazole nanocapsules use has R2 values of 0.937, 0.399, 0.899, and 0.785 and m values of 1593, 0.061, 11409, and 2.560. The Nanocapsules released the medication over 45 minutes. The ethyl cellulose and HPMC nanocapsules that contain miconazole were created under ideal circumstances and exhibit good release properties.

Targeted delivery of essential oils of Salvia officinalis L to AGS cancer cells using PLA-spermine-PEG-FA

The MTT test was used in this study to evaluate anticancer potential of Salvia officinalis L's essential oil on AGS cells. The results showed that the Salvia officinalis L's essential oil has high potential anticancer activity against AGS cells. To improve the solubility of the essential oil and its targeted administration to AGS cells, poly lactic acid-spermine-poly ethylene glycol-folic acid (PLA-Spermine-PEG-FA) (FPSP) was utilized. For this purpose, Salvia officinalis L's essential oil and silver nanoparticles were encapsulated into the PLA-Spermine-PEG-FA (FPSP) using the solvent diffusion technique. Then, using transmission electron microscope (TEM) and dynamic light scattering (DLS), respectively, morphology, zeta potential, as well as average particle size characteristics of the nanoparticles were evaluated. The FPSP/essential oil nanoparticles (FPSP/EO) were spherical in shape and had an average particle size of 200–300 nm. The mean particle dimensions for both PSP/silver/EO and FPSP/silver/EO nanoparticles assemblies are measured at 236.52 ± 22.64 nm and 248.95 ± 28.17 nm, respectively. The results showed that the zeta potential values for PSP/silver/EO and FPSP/silver/EO were −18.3 ± 0.7 mV and −20.6 ± 1.3 mV, respectively. The results of this test showed that FPSP/Silver/EO significantly reduced the percentage of AGS cell viability better than EO and PSP/Silver/EO. The best treatment in this experiment was FPSP/Silver/EO at a concentration of 50 μL/mL and time 72 h. The minimum value of IC50 in FPSP/Silver/EO was observed as 21.11 μL/mL in 72 h.

Lipid Nanoparticles Loading Steroidal Alkaloids of Tomatoes Affect Neuroblastoma Cell Viability in an In Vitro Model.

Tomato by-products represent a good source of phytochemical compounds with health properties, such as the steroidal glycoalkaloid α-tomatine (α-TM) and its aglycone tomatidine (TD). Both molecules have numerous beneficial properties, such as potential anticancer activity. Unfortunately, their therapeutic application is limited due to stability and bioavailability issues. Therefore, a valid strategy seems to be their encapsulation into Solid Lipid Nanoparticles (SLN). The nanoformulations containing α-TM (α-TM-SLN) and TD (TD-SLN) were prepared by solvent-diffusion technique and subsequently characterized in terms of technological parameters (particle size, polydispersity index, zeta potential, microscopy, and calorimetric studies). To assess the effect of α-TM and TD on the percentage of cellular viability in Olfactory Ensheathing Cells (OECs), a peculiar glial cell type of the olfactory system used as normal cells, and in SH-SY5Y, a neuroblastoma cancer cell line, an MTT test was performed. In addition, the effects of empty, α-TM-SLN, and TD-SLN were tested. Our results show that the treatment of OECs with blank-SLN, free α-TM (0.25 µg/mL), and TD (0.50 µg/mL) did not induce any significant change in the percentage of cell viability when compared with the control. In contrast, in SH-SY5Y-treated cells, a significant decrease in the percentage of cell viability when compared with the control was found. In particular, the effect appeared more evident when SH-SY5Y cells were exposed to α-TM-SLN and TD-SLN. No significant effect in blank-SLN-treated SH-SY5T cells was observed. Therefore, SLN is a promising approach for the delivery of α-TM and TD.

Formulation and Evaluation of Topical Microsponge Based Gel of Clotrimazole

The study's overarching goal is to develop a novel medication delivery method based on microsponge gel containing clotrimazole. Clotrimazole is poorly absorbed from the gastrointestinal tract (GIT), has a short half-life of only 2 h, & is metabolized into inert molecules by the liver. Therefore, clotrimazole's drug delivery method must be modified for topical application. Microsponge delivery is a novel approach to sustained drug release. Microsponges were made with a polymer solution of Eudragit RS 100 in dichloromethane (DCM) and ethanol (1:1) using a quasi-emulsion solvent diffusion technique. A number of metrics, including production yield, entrapment efficiency, particle size measurement, and in vitro drug release studies, were used to each microsponge formulation. For topical administration, the optimized microsponge formulation F6 was transformed into a gel formulation. Prepared gel was compared to a commercially available formulation based on physical factors such as pH, viscosity, spreadability, drug content, and an in vitro diffusion investigation. Most of the formulations were discrete and spherical in shape, indicating a satisfactory production yield, suggesting quasi-emulsion solvent diffusion method is a promising methodology for the fabrication of microsponge. Clotrimazole was released steadily over the course of 12 hours from the microsponge gel formulation MGI (F6). Therefore, the medicine in the form of a microsponge can reduce the risk of adverse effects and increase patient compliance by avoiding skin contact.

Formulation and Evaluation of Microsponge Gel for Topical Delivery of Antifungal Drug

The quasi emulsion solvent diffusion technique was used to create the clotrimazole microsponges, which were eventually recognized as an efficient carrier for the topical delivery of the medicine. The characteristics of the created system were significantly affected by the drug:polymer ratio. It was discovered that microsponges made for prolonged release formulation were effective, and clotrimazole microsponges with gel produced results that were equivalent. Microsponge gel compositions that were prepared beforehand showed regulated medication release. It has been shown that microsponges can transport medications for topical antifungal therapy successfully. Given how well the formulations kept the medication on the skin, it appears that microsponge gel is a more effective drug delivery mechanism than ordinary gel.

Formulation And Evaluation of Quercetin Loaded Nanosponges of Abiraterone Acetate

A novel idea in medicine delivery is the use of nanosponges. In the current research, an effort was made to create in-situ gel based on nanosponges that contained abiraterone acetate loaded with quercetin. The major purpose of nanosponges is to offer a prolonged release, lessen the negative effects of conventional dosage forms, and enhance the bioavailability of abiraterone acetate by using quercetin as a natural bioenhancer. Combining ethyl cellulose and eudragit in varying quantities, the quasi emulsion solvent diffusion technique was used to create nanosponges and quercetin as a natural bioenhancer. The formulation properties of the produced nanosponges were assessed. All batches of nanosponges had their manufacturing yield and trapping effectiveness assessed. Formulations F 03-P1 and F 07-P2 were found to be the optimum formulations based on results. Both F 03- P1 and F 07-P2 were used to create the gels G1 and G2. Viscosity, spreadability, drug content, and in-vitro tests showing 28.88% drug release after 24 hours all favored G2 as the optimal formulation. A gel base was created using the optimized formulation after it had been tested for scanning electron microscopy (SEM) analysis. Nanosponges containing gel had evaluated for different tests. According to the study, adding drugs to nanosponges can increase the rate of drug release, improve medication targeting at a particular spot, and hence lessen systemic toxicity.

Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation

BackgroundThe objective of the present investigation was to obtain directly compressible agglomerates of ibuprofen with nicotinamide by a quasi-emulsification solvent diffusion technique. Ibuprofen-nicotinamide agglomerates were prepared by quasi-emulsification solvent diffusion technique using ethanol (good solvent), water (poor solvent), and chloroform (bridging liquid). The prepared agglomerates were characterized by ATR-FTIR, powder X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy and were evaluated for tableting performance and in vitro drug release. To appropriately identify the hydrogen bonding sites, a thorough understanding of the structures of API and coformer is necessary, hence molecular docking approach was implemented to depict the interaction between the proposed coformer and COX-2 protein (PDB Id:4PH9).ResultsThe percent yield of agglomerates was in the range of 85–98 w/w%, and drug content for all batches was in the range of 96–99%. The microphotographs showed irregular circularly shaped agglomerates. ATR-FTIR study showed a strong possibility of hydrogen bonding between ibuprofen and nicotinamide. The crystallinity of ibuprofen was slightly reduced and confirmed by P-XRD and DSC. Crushing strength and friability studies showed good handling qualities of ibuprofen agglomerates. Heckel plot studies showed low mean yield pressure and high tensile strength, indicating excellent compressibility and compactibility of ibuprofen agglomerates. More than 90% drug release was obtained within 60 min in PBS (pH 7.4). The docking studies revealed that nicotinamide individually has –CDOCKER energy 16.8109 where coformer showed 29.0584, which indicates coformer has a better binding affinity to target as compared to nicotinamide individual.ConclusionsIt can be concluded that the agglomerates improved the dissolution, tableting performance, and solid-state properties of ibuprofen and hence can be useful to improve the therapeutic performance of ibuprofen.Graphic

Development of Clindamycin Loaded Oral Microsponges (Clindasponges) for Antimicrobial Enhancement: In Vitro Characterization and Simulated in Vivo Studies.

Clindamycin phosphate (CLP) is a broad-spectrum antibiotic that is used widely for different types of infections. It has a short half-life and hence it should be taken every six hours to ensure adequate antibiotic blood concentration. On the other hand, microsponges are extremely porous polymeric microspheres, offering the prolonged controlled release of the drug. The present study aims to develop and evaluate innovative CLP-loaded microsponges (named Clindasponges) to prolong and control the drug release and enhance its antimicrobial activity, consequently improving patient compliance. The clindasponges were fabricated successfully by quasi-emulsion solvent diffusion technique using Eudragit S100 (ES100) and ethyl cellulose (EC) as carriers at various drug-polymer ratios. Several variables were optimized for the preparation technique including the type of solvent, stirring time, and stirring speed. The clindasponges were then characterized in terms of particle size, production yield, encapsulation efficiency, scanning electron microscopy, Fourier Transform Infrared Spectroscopy analysis, in vitro drug release with kinetic modeling, and antimicrobial activity study. Moreover, in vivo, pharmacokinetics parameters of CLP from the candidate formula were simulated based on the convolution method and in vitro-in vivo correlation (IVIVC-Level A) was built up successfully. Uniform spherical microsponges with 82.3 µm mean particle size with a porous spongy structure were evident. ES2 batch exhibited the highest production yield and encapsulation efficiency (53.75 and 74.57%, respectively) and it was able to exhaust 94% of the drug at the end of 8 h of the dissolution test. The release profile data of ES2 was best fitted to Hopfenberg kinetic model. ES2 was significantly (p < 0.05) effective against Staphylococcus aureus and Escherichia coli compared to the control. Also, ES2 displayed a twofold increase in the simulated area under the curve (AUC) compared to the reference marketed product.

Effect of Different Stabilizers on Spherical Agglomerates of Montelukast Sodium by Quasi Emulsion Solvent Diffusion (QESD)

Abstract: The present study was focused on the spherical crystallization of an asthmatic drug, Montelukast Sodium (MLS) using quasi emulsion solvent diffusion (QESD) technique in which distilled water was an external phase and the internal phase consisted of Ethanol which acts as good solvent and Ethyl acetate as a bridging liquid for recrystallization and agglomeration process. Apart from being poorly water soluble, MLS exhibits poor flow and compressibility. The spherical agglomeration was carried out in the presence of different stabilizers like acacia, PEG 4000, sodium lauryl sulphate, span 40 and tween 80. The prepared agglomerates were characterized in terms of production yield, drug content, solubility, in-vitro release profile, Xray diffraction (XRD), and Fourier transform infra red spectroscopy (FT-IR).The optimized spherical agglomerates exhibited excellent physicochemical and micromeritic properties, solubility and dissolution rate when compared with pure drug .The XRD also revealed a characteristic decrease in crystallinity. The dissolution studies demonstrated a marked increase in the dissolution rate. FTIR study reveals there are no chemical changes in prepared recrystallized agglomerates. The considerable improvement in the dissolution rate of MLS from optimized crystal formulation was attributed to the wetting effect of polymers, decreased drug crystallinity, altered surface morphology and micronization. If this process can be scaled-up to manufacturing level, this technology has the potential to provide the directly compressed spherical agglomerates with improving the physicochemical and micromeritic properties

Development and Characterization of Polymeric Microsponge as a New Vehicle to Deliver Urea Topically.

Topical delivery of therapeutic agents is considered beneficial due to various advantages like ease of administration, avoidance of the first-pass effect, and improved patient compliance. Therefore, scientists around the globe are exploring this route for the delivery of drugs nowadays. The present patent investigation aimed to prepare, optimize, and characterize the urealoaded microsponges for efficient topical delivery in vitro. Urea-loaded ethylcellulose microsponges were prepared using quasi emulsion solvent diffusion technique and optimized using Box-Behnken design (BBD). Furthermore, they were characterized in-vitro using various techniques like scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), and X-ray diffraction analysis (XRD). In-vitro drug release and release kinetics analysis was also performed. Urea-loaded microsponges were spherical and porous. Optimized urea loaded microsponges showed a minimum size (39.78 ± 1.98 μm), high entrapment (74.56 ± 2.8%), acceptable polydispersity index (PDI) (0.224 ± 0.081) and zeta potential (-21.9 ± 2.9 mV). These microsponges were capable of sustaining the release of urea for 24 h (91.21 ± 5.20%), and the mechanism of release was the combination of diffusion and erosion. The developed microsponge system could be beneficial for topical delivery of urea as it could reduce the dosing frequency of urea and increase patient compliance through its sustained release.

Exploring potential of diacerin nanogel for topical application in arthritis: Formulation development, QbD based optimization and pre-clinical evaluation

Diacerein (DCN) is a chondroprotective agent which shows inadequate oral bioavailability along with gastrointestinal side effects. This study is intended to develop a topical novel DCN delivery system. DCN nanogel was prepared by emulsion solvent diffusion technique. The formulation was optimized by response surface methodology by taking two independent variables, concentration of carbopol 940 and eudragit RSPO and three dependent variables, particle size, % entrapment efficiency (EE) and % drug release at 24 h. The optimized formulation had adequat% EE, % drug release at 24 h and particle size. The particle size for optimized nanogel was 190.3 nm with % EE of 83.51% whereas % drug release at 24 h was found 90.13%. The optimized DCN nanogel was analyzed by differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (DTIR) and transmission electron microscopy (TEM) studies. The drug release kinetic study has shown that the gel followed Higuchi’s model and the diffusion was anomalous in nature. The nanogel was characterized for physical examination, viscosity, homogeneity and stability parameters and the results obtained were found upto the mark. The ex-vivo permeation study data was in correlation with results of in-vitro study. In-vivo anti-arthritic study proved the efficacy of developed formulation for arthritis in Freund’s Adjuvant Arthritic model. This research work has proved the significant potential of innovated product for arthritis by topical route, as it overcomes the drawbacks of oral route, highly efficient, sustained and targeted the release of drug without any accumulation and toxicity.

DEVELOPMENT AND EVALUATION OF MICROSPONGE GEL OF AN ANTIFUNGAL DRUG

Objective: The objective of the present study was to compare the release effect of Luliconazole from different polymeric (Hydrophilic and Hydrophobic) microsponges prepared using varying concentrations. The best microsponge was selected and incorporated into different gel (Natural and synthetic) and drug release is determined and compared with marketed formulation.&#x0D; Methods: Polymers such as EC, HPMC, Eudragit RSPO and PVA as emulsifier, and solvent DCM is used as solvent. Microsponge were prepared by using the quasi emulsion solvent diffusion technique. FTIR was studied to estimate the incompatibility. Microsponges were evaluated for SEM, particle size, drug content, and In vitro diffusion studies. Optimized microsponge incorporated gel was prepared by using different gel (flax seed gel and Aerosil gel) were evaluated for pH, spreadability, extrudability, drug content and in vitro diffusion studies.&#x0D; Results: Theresults obtainedshowed no physical-chemical incompatibility between the drug and the polymers. EC, HPMC and EC combination was found to be a suitable polymer compared to Eudragit RSPO and other combination in preparation of microsponge. From the evaluation of microsponge, the optimized F1 formulations was incorporated into different gel (flax seeds, aerosil) and compared with marketed formulation in which MG-I (flax seed gel) was considered as good topical anti-fungal microsponge gel based on there physical parameters and drug release kinetics.&#x0D; Conclusion: Microsponge and microsponge gel were successfully prepared for Luliconazole and their evaluation studies of each dosage form revealed that topically applied microsponge gel possess immense potential to control the release rate of medicament to improve the bioavailability as well as patient compliance.

Curcumin-Loaded Chitosan Nanoparticle Preparation and Its Protective Effect on Celecoxib-induced Toxicity in Rat isolated Cardiomyocytes and Mitochondria.

Curcumin has a wide range of pharmacological activities, including antioxidant, anti-inflammatory and tissue protective. In here we hypothesized that curcumin-loaded chitosan-coated solid lipid nanoparticles (CuCsSLN) are able to increase its overall bioavailability and hence its antioxidant and mitochondria;/lysosomal protective properties of curcumin. CuCsSLN were prepared using solvent diffusion technique for formation of solid lipid nanoparticles (SLNs) and electrostatic coating of positive-charged chitosan to negative surface of SLNs. CuCsSLN showed the encapsulation efficiency of 91.4±2.7%, the mean particle size of 208±9 nm, the polydispersity index of 0.34±0.07, and the zeta potential of+53.5±3.7 mV. The scanning electron microscope (SEM) images of nanoparticles verified their nanometric size and also spherical shape. Curcumin was released from CuCsSLN in a sustain release pattern up to 24 hours. Then isolated cardiomyocytes and mitochondria were simultaneously treated with (1) control (0.05% ethanol), (2) celecoxib (20 µg/ml) treatment, (3) celecoxib (20 µg/ml)+++CuCsSLN (1 µg/ml) treatment, (4) CuCsSLN (1 µg/ml) treatment, (5) celecoxib (20 µg/ml)+++curcumin (10 µM) treatment and (6) curcumin (10 µM) treatment for 4 h at 37°C. The results showed that celecoxib (20 µg/ml) induced a significant increase in cytotoxicity, reactive oxygen species (ROS) formation, mitochondria membrane potential (ΔΨm) collapse, lipid peroxidation, oxidative stress and mitochondrial swelling while CuCsSLN and curcumin reverted the above toxic effect of celecoxib. Our data indicated that the effect of CuCsSLN in a number of experiments, is significantly better than that of curcumin which shows the role of chitosan nanoparticles in increasing effect of curcumin.

Development of a Polymeric Membrane Impregnated with Poly-Lactic Acid (PLA) Nanoparticles Loaded with Red Propolis (RP).

The main objectives of this study were to develop and characterize hydrophilic polymeric membranes impregnated with poly-lactic acid (PLA) nanoparticles (NPs) combined with red propolis (RP). Ultrasonic-assisted extraction was used to obtain 30% (w/v) red propolis hydroalcoholic extract (RPE). The NPs (75,000 g mol−1) alone and incorporated with RP (NPRP) were obtained using the solvent emulsification and diffusion technique. Biopolymeric hydrogel membranes (MNPRP) were obtained using carboxymethylcellulose (CMC) and NPRP. Their characterization was performed using thermal analysis, Fourier transform infrared (FTIR), total phenols (TPC) and flavonoids contents (TFC), and antioxidant activity through the radical scavenging assay with 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) and Ferric reducing antioxidant power (FRAP). The identification and quantification of significant RP markers were performed through UPLC-DAD. The NPs were evaluated for particle size, polydispersity index, and zeta potential. The TPC for RPE, NPRP, and MNPRP was 240.3 ± 3.4, 191.7 ± 0.3, and 183.4 ± 2.1 mg EGA g−1, while for TFC, the value was 37.8 ± 0.9, 35 ± 3.9, and 26.8 ± 1.9 mg EQ g−1, respectively. Relevant antioxidant activity was also observed by FRAP, with 1400.2 (RPE), 1294.2 (NPRP), and 696.2 µmol Fe2+ g−1 (MNPRP). The primary markers of RP were liquiritigenin, isoliquiritigenin, and formononetin. The particle sizes were 194.1 (NPs) and 361.2 nm (NPRP), with an encapsulation efficiency of 85.4%. Thermal analysis revealed high thermal stability for the PLA, nanoparticles, and membranes. The DSC revealed no interaction between the components. FTIR allowed for characterizing the RPE encapsulation in NPRP and CMC for the MNPRP. The membrane loaded with NPRP, fully characterized, has antioxidant capacity and may have application in the treatment of skin wounds.

Formulation of Solid Lipid Nanoparticles Loaded with Nociceptin/Orphanin FQ (N/OFQ) and Characterization in a Murine Model of Airway Hyperresponsiveness

Asthma is characterized by chronic inflammation and a variable degree of airway hyperresponsiveness (AHR). Our previous papers documented a role for Nociceptin/Orphanin FQ (N/OFQ) and its receptor N/OFQ peptide (NOP) in AHR. Therefore, the aim of this study was to improve the bioavailability of N/OFQ by developing solid lipid nanoparticles (SLNs). N/OFQ-loaded SLNs were prepared by the Quasi Emulsion Solvent Diffusion (QESD) technique and then characterized. Brown Norway rats were sensitized to ovalbumin (OVA) and treated with an intratracheal administration of saline solution or N/OFQ-SLN. Then, 24 h after the last challenge, functional histological and molecular evaluations were performed. SLNs showed a mean diameter of 233 ± 0.03 nm, a polydispersity index (PDI) value around 0.28 ± 0.02 and a drug release percentage of 84.3. The in vitro release of N/OFQ from SLNs showed that the release of the peptide starts already after two hours of incubation. Animals receiving N/OFQ-SLN showed a significative decrease in allergen-induced AHR compared to the control group. These results showed the positive effects of N/OFQ-SLNs on the inflammatory process and on the mechanical properties of the airways, suggesting that the innovative nanotechnological approach may be therapeutically beneficial for asthmatic patients.