Drug-polymer Ratio Research Articles

ADVANCING TOPICAL POSACONAZOLE DELIVERY: BOX BEHNKEN DESIGN MICROSPONGE HYDROGEL OPTIMIZATION AND EXTENSIVE IN VIVO INVESTIGATION

Objective: The primary aim of this study was to develop a novel hydrogel formulation containing Posaconazole (PCZ) encapsulated within microsponges. Furthermore, the study aimed to assess the permeation properties of this formulation in vivo using a mouse model. Methods: To achieve this aim, a series of seventeen trials were conducted using the Box Behnken Design methodology. These trials were designed to optimize the production of PCZ Microsponges (PCZ MS), which were subsequently incorporated into a hydrogel matrix. Skin permeation studies were then performed to evaluate the ability of the PCZ microsponge-based hydrogel to deliver the drug across the skin barrier. These studies involved comparison with a standard hydrogel formulation lacking microsponges. Results: This study assessed the efficacy of microsponge gel formulation PM-3 for drug entrapment, yield, and sustained release compared to a conventional gel. PM-3 displayed the highest entrapment efficiency of 98.5% and a yield of 95.62%, indicating a direct correlation with the 1:1 drug-polymer ratio. Moreover, PM-3 exhibited sustained drug release over 12 h, releasing 83.82% of PCZ compared to 65.31% with the normal gel, suggesting its potential for prolonged therapeutic action. These findings underscore the promise of microsponge-based hydrogels, like PM-3, in enhancing therapeutic outcomes through sustained drug release, warranting further exploration for clinical applications. Conclusion: The findings of this study highlight the promising potential of microsponge-based hydrogels as effective carriers for localized drug delivery, particularly in the context of treating skin fungal infections.

In vitro Characterization and Drug Release Studies of Ethambutol-Loaded Nanoparticles for Pulmonary Delivery

Background: The development of more effective drug delivery techniques is necessary to increase treatment efficacy and patient compliance since tuberculosis (TB) is still a serious worldwide health concern. Ethambutol is a vital aspect of TB treatment, and using nanoparticles to carry it to the lungs may provide targeted delivery and prolonged release, which might enhance the effectiveness of the treatment. Objective: This work aimed to optimize the formulation for prolonged drug release by synthesizing and assessing ethambutol-loaded nanoparticles using the desolation technique with albumin as the polymer. Additionally, the effects of different drug-polymer ratios and stirring rates were investigated. Methods: Nine formulations of ethambutol-loaded nanoparticles were prepared by varying the drug-polymer ratios (1:1 to 1:2) and stirring speeds (500 to 1500 rpm). Key parameters, such as particle size, drug entrapment efficiency, and zeta potential, were measured. The optimized formulation was selected based on the smallest particle size and highest drug entrapment efficiency. Scanning electron microscopy was used to analyze the surface morphology of the nanoparticles. The in vitro drug release profile of the optimized formulation was studied over 24 hours. Results: Increasing the drug-polymer ratio from 1:1 to 1:2 increased nanoparticle size from 192.1 nm to 605.06 nm and decreased drug entrapment efficiency from 75.7%±0.08 to 34%±0.06. Higher stirring speeds (500 to 1500 rpm) also led to larger particle sizes and reduced drug entrapment due to polymer self-aggregation. Zeta potential values ranged from -5.56 to -25.6 mV. Scanning electron microscopy confirmed smooth, spherical nanoparticles. The optimized formulation, EN-5, exhibited the smallest particle size and highest drug entrapment efficiency. In vitro drug release studies showed a sustained ethambutol release, with 42.66±1.53% released in 12 hours and 79.082±2.98% in 24 hours. Conclusion: Ethambutol-loaded nanoparticles having the ability to transport drugs to the lungs over an extended period of time were developed and optimized in the study. With improved drug delivery systems, the optimized formulation showed notable drug entrapment efficiency and controlled release, suggesting its potential to improve tuberculosis therapy.

Release Kinetic of Sustained Release Matrix Tablet of Linezolid Containing Polymer Blend.

Tuberculosis (TB) is a bacterial infection mainly affecting the lungs. TB is a major health problem worldwide and the occurrence of extensively drug-resistant TB (XDR-TB) and multidrug-resistant TB (MDR-TB) offers considerable hurdles to effective treatment and disease management. The growth of treatment-resistant Mycobacterium TB strains has prompted the investigation of alternate therapeutic techniques, including the application of sustained drug delivery. Sustained-release drugs reduce the need for frequent dosing can extend the effects of linezolid by 8 to 12 hours, thus improving the patient’s adherence to the treatment. The objective of this study is to formulate oral sustained-release linezolid tablets employing blends of polymers like hydroxy propyl methyl cellulose (HPMC)- K100M, ethyl cellulose, xanthan gum, and chitosan to provide sustained drug release. Linezolid was made into a sustained-release tablet by employing the direct compression method using different drug-polymer ratios. Formulated tablets were compared with marketed formulations to assess the similarity factor. The formulation was assessed for drug-excipient interaction, solubility, flow properties, etc. The diameter, friability, thickness, hardness, weight variation, in-vitro drug release, and drug release kinetics of compressed tablets were examined. Drug release research proved that all polymers were able to sustain drug release. Formulation (F5) with HPMC (100mg) and ethyl cellulose (100mg) resulted in 49.89% drug release after 8 hours, making it the optimal formulation. According to the kinetic model of the drug release, the Higuchi model was selected, which indicates the diffusion of the drug from an insoluble matrix. The optimized formulation showed a similarity factor of 52% with the marketed formulation, suggesting similarity in drug release between these two formulations.

Formulation Development and Evaluation of Transdermal Patches of Apigenin.

Apigenin is a flavonoid that is abundantly present in fruits and vegetables. It has a diverse range of therapeutic properties, including cardioprotective, neuroprotective, analgesic, and cancer-preventive effects. Its safety profile, even at higher doses, makes the compound particularly valuable. Apigenin, along with excipients, was used to formulate patches using the solventcasting method on a glass mold. Seven distinct batches of patches were formulated using different combinations of polymers. The drug-polymer ratios employed in these formulations were (1:2), (1:3), (1:4), (1:4), (1:(2:8), (1:(1:9), and (1:(2:8) for both drugs. The formulated patches were evaluated and results indicate that the transdermal patches (TP5) have promising results.

Formulation Variables Influencing the Development of Ketoconazole Gastroretentive Drug Delivery System

Background: Ketoconazole (KZ) is categorized as class II according to the Biopharmaceutics Classification System (BSC) classification, which shows a strong pH-dependent solubility where its solubility is enhanced under an acidic medium (pH below 3). This strong pH dependence results in unpredictable absorption and a wide range of bioavailabilities. Objective: To prolong the gastric residence time of KZ’s tablet to enhance KZ’s solubility and hence its bioavailability for better therapeutic activity. Methods: To prepare mucoadhesive tablets, we use both direct and wet granulation methods. We employed various evaluation tests to assess the prepared tablets. These tests encompass a range of assessments, including weight variation, hardness, thickness, friability, disintegration test, swelling study, mucoadhesive strength study, and in vitro drug release studies. Results: The study found that polymer viscosity, as well as polymer concentration, have a significant effect on mucoadhesive strength and drug release, whereas diluent type has a non-significant influence on drug release. We selected Formula 7, which employs xanthan gum as a mucoadhesive polymer in a 1:1 drug polymer ratio, as the optimum formula because it provides an accepted physico-mechanical property and releases 87% of the drug over 8 hours. Conclusions: Gastric mucoadhesive tablets may be an effective method of delivering active ingredients, as they provide a favorable environment that enhances their dissolution by extending their duration in the stomach, thereby increasing their bioavailability.

Polymeric liposomes of emtricitabine employing modified pullulan—an attempt to reduce associated hepatotoxicity

Emtricitabine (FTC) a BCS class I drug, is used for HIV prevention. The high solubility of the drug is the leading cause of severe hepatotoxicity and lactic acidosis. This research focuses on the use of modified pullulan for the preparation of polymeric liposomes of FTC. Modified pullulan was synthesized using cholesterol, and succinic anhydride in a controlled chemical environment. The formation of the polymer was established through analysis of spectra. Varying the drug-polymer ratio (1:1, 1:2, and 1:3), the drug-polymer composite was loaded in the vesicular system of soya phosphatidylcholine and cholesterol. Formulations were evaluated for drug entrapment, particle size, surface morphology, and in vitro and ex vivo drug release. An in vivo study of the pure drug and the best formulation on mice was conducted for 28 days following daily oral administration to evaluate the effect on liver and hematological parameters. The best formulation was further subjected to cytotoxicity study on hepatic cell lines. Spectral analysis confirmed the formation of modified pullulan. All formulations showed high drug entrapment in the nanovesicles. The in vitro and ex vivo drug release profiles depicted a controlled release of the drug. Hematological parameters were found to be under control in the animals throughout the experimentation. A comparative histopathology study on the livers and cytotoxicity study on hepatic cell lines revealed the safety of the best formulation over the pure drug. Hence it can be concluded that polymeric liposomes of FTC can be a promising mode of delivery to overcome its limitations.

Impact of Methods of Preparation on Mechanical Properties, Dissolution Behavior, and Tableting Characteristics of Ibuprofen-Loaded Amorphous Solid Dispersions.

This study aims to improve the biopharmaceutical, mechanical, and tableting properties of a poorly soluble drug, ibuprofen (IBP), by preparing amorphous solid dispersion (ASD) followed by a sustained-release tablet formulation. A suitable polymer to develop an ASD system was chosen by utilizing the apparent solubility of IBP in various polymer solutions. ASDs containing various ratios of IBP and selected polymer were prepared by the melt fusion (MF) method. ASD containing optimized drug-polymer ratio prepared by freeze-drying (FD) method was characterized and compared physicochemically. The solubility of IBP in water increased 28-fold and 35-fold when formulated as ASD by MF and FD, respectively. Precise formulations showed amorphization of IBP and increased surface area, improving solubility. The dissolution pattern of optimized ASD-IBP in pH 6.8 phosphate buffer after 60 min in MF and FD was enhanced 3-fold. In addition, direct compression tablets comprising optimized ASD granules from MF and FD were made and assessed using compendial and noncompendial methods. ASD-IBP/MF and ASD-IBP/FD formulations showed a similar drug release profile. In addition, 12 h of sustained IBP release from the ASD-IBP-containing tablets was obtained in a phosphate buffer with a pH of 6.8. From the dissolution kinetics analysis, the Weibull model fitted well. The drug release pattern indicated minimal variations between tablets formed using ASD-IBP prepared by both procedures; however, pre- and postcompression assessment parameters differed. From these findings, the application of ASD and sustained-release polymers in matrix formation might be beneficial in improving the solubility and absorption of poorly soluble drugs such as IBP.

Development, characterization, and in-vivo evaluation of a novel chitosan: Guar gum particulate system for colonic release of triamcinolone

Drug delivery systems based on carbohydrate polymers have shown promising results for the colonic release of drugs due to the selective degradation by the local microbiota and physical resistance to the physiological conditions of the gastrointestinal tract. This work aimed to obtain and characterize a novel particulate system (PS) based on chitosan and guar gum polymers (CHI-GG) for the release of triamcinolone (TRI) and evaluate the in vivo anti-inflammatory activity of ulcerative colitis. PS were prepared by combining coacervation and spray drying techniques using different CHI-GG and drug-polymer ratios. For obtained, PS CHI-GG-TRI systems were characterized. To evaluate the in vivo activity of PS containing TRI, we used Wistar rats to observe the anti-inflammatory response in macroscopic and microscopic parameters of the intestinal mucosa. PS-TRI demonstrated improvements in the aspects related to reducing adverse effects of the drugs when administered in their free form. PS-TRI release occurred in only 69 % of the active in 24 h; the macro and microscopic parameters and the activity of the experimental ulcerative colitis were softened, and an excellent potential anti-inflammatory effect was observed. Infrared data evidenced the incorporation of TRI on the PS. DSC analysis showed the compatibility between TRI and the polymers of the PS. The release kinetics showed an initial burst release of TRI followed by a controlled release profile for up to 30 h. Therefore, a new PS for TRI release was obtained that can swell and control TRI release and that showed anti-inflammatory activity in an animal model, also reducing adverse effects present in conventional treatments.

Formulation and characterization of ibuprofen solid dispersions using native and modified starches

Background: Ibuprofen is an anti-inflammatory analgesic drug that is weakly water-soluble with a poor bioavailability.Objectives: The aim of this study is to formulate ibuprofen solid dispersions by solvent evaporation method using natural polymers (native cassava and genetically modified cassava (GMS), Cassava nanocrystal and corn starches) as possible hydrophilic carriers at varying weight proportions to optimize ibuprofen solubility and dissolution.Material and Methods: Solvent evaporation method was used to formulate the ibuprofen solid dispersions at different drug polymer ratios. The pure drug and solid dispersions were characterized using Scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffractometer (XRD), particle size, and in vitro drug release.Results: Solid dispersions formulated with starch nanocrystals showed the highest solubility. All solid dispersions prepared with drug:polymer ratio 1:2 generally showed highest solubility. According to the FTIR, the chemical structure of ibuprofen remained intact in the amorphous solid dispersion, but the structure changed from crystalline to amorphous, according to the XRD and the DSC also confirmed this. The scanning electron microscopy showed the solid dispersions were more porous than the pure drug. Higher dissolution rate was observed with nanocrystal solid dispersions with T50 (time required for 50% of the medication to be released) between 1.8 and 4.1 minutes.Conclusion: This study has shown that using these natural polymers increased the solubility and dissolution rate of ibuprofen.

Preparation and evaluation of naproxen ternary solid dispersion using genetically modified cassava starch and hydroxypropyl methyl cellulose

Background: Naproxen has poor aqueous solubility and high permeability, making its formulation into oral dosage form challenging. The objective of this work was to enhance naproxen aqueous solubility by formulating it into solid dispersion (SD) using genetically modified cassava starch (GMCS) and hydroxypropyl methyl cellulose (HPMC) as polymers, and polysorbate-80 as surfactant.Materials and Methods: Naproxen SD was prepared by solvent evaporation. Different polymer-drug ratios (1:1, 2:1, 3:1 and 4:1) were used. The SDs were evaluated for solubility and the optimum formulation (S2) subjected to Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Pure naproxen tablets (TN) and S2 tablets (T2) were directly compressed and assessed for hardness, friability, weight uniformity, disintegration and dissolution times.Results: The SD of polymer/drug ratio 2:1 and GMCS/HPMC proportion 2:1 had the highest solubility with the polymers showing synergism. Incorporating polysorbate-80 improved solubility by over 20 folds. SEM micrograph of the SD appeared smooth and spherical. DSC thermogram indicated a reduction in crystallinity of naproxen. FTIR spectrum showed no evidence of interaction with the polymers. T2 and TN tablets showed acceptable hardness, disintegration time and weight uniformity. The t50 and t90 dissolution values for T2 were 4.9 and 37.7 minutes respectively which were considerably lower than that of TN (28.57 and 63.42 minutes).Conclusion: Naproxen solubility was enhanced by solid dispersion formulation using genetically-modified cassava starch/HPMC blend. Synergistic effect in the improvement of naproxen solubility was established between the polymers. Inclusion of polysorbate-80 also improved naproxen solubility in the solid dispersion.

The Role of Nanoparticles in Sunscreen: UV Protection and Particle Size

Sunscreen formulas are essential for protecting the skin from damaging UV rays, which reduces the risk of sunburn, skin cancer, and premature aging. However, conventional sunscreens frequently lack further advantages including anti-aging and antioxidant capabilities. Strong polyphenolic component epigallocatechin-3-gallate (EGCG), present in green tea extracts, has anti-inflammatory, antioxidant, and photoprotective properties. Similar to this, poly amino acids and hyaluronic acid (HA) have hydrating, anti-aging, and skin-repairing qualities. In this work, we investigated the co-delivery of EGCG and HA/poly amino acids in sunscreen formulations using nano-carriers, namely transferosomes and polymeric nanoparticles. To increase the effectiveness of these nano-carriers, a number of formulation factors, such as the drug-polymer ratio, surfactant concentration, homogenization speed, and sonication time, were improved. When compared to normal EGCG solutions, the optimized nano-formulations showed superior properties such reduced particle size, higher encapsulation efficiency, and improved skin permeability. Studies on cytotoxicity showed that the nano-formulations were not harmful to skin cells and that they increased cell viability when compared to EGCG in its purest form. Because the nano-formulations contained EGCG and HA/poly amino acids, they offered considerable protection against skin damage caused by UV radiation. The spherical shape of the nano-carriers was shown by transmission electron microscopy, and the lack of interactions between EGCG and excipients was validated by differential scanning calorimetry and Fourier-transform infrared spectroscopy.

Formulation and Evaluation of Solid Dispersion of Felodipine by Hot Melt Extrusion for Enhancement of Solubility

ABSTRACT Background: Felodipine (BCS Class II) undergoes extensive first-pass metabolism with bioavailability of about 15% that creates problem in therapeutic efficacy after oral administration. Objective: Immediate release formulation of felodipine was developed using hot-melt extrusion (HME) technique in an attempt to improve solubility and dissolution of felodipine through the solid dispersion technique. Materials and Methods: The solid dispersion was prepared using Eudragit EPO, NE30D as a carrier with different drug polymer ratios using the HME technique. The optimized batch was made into tablets. The solid dispersion was characterized by solubility studies, drug content, and in vitro dissolution rate studies. Results: From the cumulative dissolution profile, it was observed that the drug and Eudragit EPO alone have the highest percentage of drug release compared to the other combinations of drug and Eudragit EPO, NE30D. It is also evident from the dissolution profile that with increase in the concentration of Eudragit NE30D, there is a decrease in the dissolution rate. There was a significant decrease in drug release even with increase in stabilizer in a smaller ratio. The dissolution profile showed that there is not much variation in the release profile of the solid dispersion alone and the solid dispersion tablets. Conclusions: Solid dispersion by the HME technique is an effective method to increase the dissolution rate of felodipine.

Targeting Breast Cancer: Encapsulation and In-vitro Studies of α-Amyrin from Capparis zeylanica L.

Historically, Capparis zeylanica L. has garnered attention for its potential effectiveness in treating cancer. This has inspired the researchers to delve into the plant’s properties in search of new and innovative compounds with anticancer properties. Therefore, the current study aimed to encapsulate and characterize α-amyrin phytochemical from leaf extract of C. zeylanica L. and study it for the in-vitro cancer cell line. The high-performance liquid chromatography (HPLC) method development of C. zeylanica L. extracts furnished α-amyrin, whose characterization was established by high-performance liquid chromatography (HPLC), fourier-transform infrared spectroscopy (FTIR), liquid chromatography-mass spectrometry (LC-MS). Molecular docking was performed using Auto Dock Vina software to validate the mechanism of action. The α-amyrin nanosponges was synthesized through the emulsion solvent diffusion method, employing various drug-polymer ratios ranging from 1:1 to 1:5, with pullulan as the chosen polymer. Compatibility was revealed no interaction using FTIR. The cytotoxic properties were assessed on MCF-7 cell lines using MTT assay. The production yield and entrapment efficiency of F1-F5 batches in the range of 43 to 68.36% and 70 to 82.5%, respectively. Batch F5 showed the highest production yield, and entrapment efficiency. The average particle size ranges from 241.3 to 603.2 nm. The F5 formulation had shown the highest drug release (90.40 ± 0.88%). The IC50 value for optimized formulation was 34.54 μg/mL as observed in MCF-7 breast cancer, which was considerable as compared with 5-fluorouracil. In-silico studies revealed that α-amyrin showed good binding affinity to breast cancer PDBIDs and form a stable complex. In our study, α-amyrin has been successfully extracted and further validation through pharmaceutical formulation was done and warranted to solidify its potential as an effective anticancer agent.

Formulation of Letrozole-loaded Ethyl Cellulose and Eudragit S100 Nanoparticles by Nanoprecipitation Technique and Determination of Cytotoxic Activity by MTT Assay

Introduction:: The major goal of this work is to develop letrozole nanoparticles using the polymer precipitation technique. Formulations were prepared by using Ethyl cellulose and Eudragit S100 as polymers. Methods:: By varying drug-polymer ratios, a total of ten formulations were prepared. By altering the drug concentration to polymer, five formulations were prepared with Ethyl cellulose and five with Eudragit S100. All ten formulations were evaluated for different characterization and evaluation parameters such as Entrapment efficiency, Loading capacity and in vitro drug release studies, particle size, stability (zeta potential), surface morphology, and drug-polymer interaction study. Result:: In comparison, the NEC 2:1 formulation showed the smallest particle size,high stability, good entrapment efficiency, and sustained drug release. This formulation was further studied to determine the anticancer activity in vitro in the MCF-7 Breast cancer cell line by MTT assay. The results indicated that the prepared formulation exhibited anticancer activity with an IC50 value of 91.26 micromolar. Conclusion:: Comparatively, Ethyl cellulose was proven to be a better polymer than Eudragit S100, and the nanoprecipitation technique was considered the most suitable technique for preparing letrozole nanoparticles.

Unveiling the potential of microsponges: Enhancing oral bioavailability

Oral medication administration is widely recognized as the most practical and widely used method. Medications with a short half-life and easy absorption in the gastrointestinal tract are quickly removed by the bloodstream. To avoid these issues, oral controlled-release formulations have been created. There are a ton of novel formulation approaches in the realm of medication delivery systems. One new novel approach that is becoming increasingly well-liked these days is the usage of microsponges. A wide variety of active chemicals can be entrapped by the highly cross-linked, porous, polymeric structure that makes up the Microsponges Delivery System (MDS). Various polymers like ethyl cellulose, polystyrene, etc., have been utilized in forming microsponges and these active microsponges can be incorporated into formulations, such as capsules, gel, and powders, and have a broad package of benefits. The microsponges have satisfactory stability over pH values ranging from 1 to 11, they exhibit reasonable stability at temperatures as high as 130, and entrapment efficiency is great, reaching 50–60%. The preparation of microsponges involves the Quasi-emulsion solvent method, and the emulsion solvent diffusion method the release of drug through microsponges increases with increasing drug-polymer ratio and lowering polymer wall thickness. The microsponges are characterized for visual characterization, zeta potential, entrapment efficiency, and drug content. This review is focused on their advantages over other dosage forms, methods of preparation, characterization, and application of microsponges.

Vancomycin and nisin-modified magnetic Fe3O4@SiO2 nanostructures coated with chitosan to enhance antibacterial efficiency against methicillin resistant Staphylococcus aureus (MRSA) infection in a murine superficial wound model

BackgroundThe objective of this research was to prepare some Fe3O4@SiO2@Chitosan (CS) magnetic nanocomposites coupled with nisin, and vancomycin to evaluate their antibacterial efficacy under both in vitro and in vivo against the methicillin-resistant Staphylococcus. aureus (MRSA).MethodsIn this survey, the Fe3O4@SiO2 magnetic nanoparticles (MNPs) were constructed as a core and covered the surface of MNPs via crosslinking CS by glutaraldehyde as a shell, then functionalized with vancomycin and nisin to enhance the inhibitory effects of nanoparticles (NPs). X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FT-IR), field emission scanning electron microscope (FE-SEM), vibrating sample magnetometer (VSM), and dynamic light scattering (DLS) techniques were then used to describe the nanostructures.ResultsBased on the XRD, and FE-SEM findings, the average size of the modified magnetic nanomaterials were estimated to be around 22–35 nm, and 34–47 nm, respectively. The vancomycin was conjugated in three polymer-drug ratios; 1:1, 2:1 and 3:1, with the percentages of 45.52%, 35.68%, and 24.4%, respectively. The polymer/drug ratio of 1:1 exhibited the slowest release rate of vancomycin from the Fe3O4@SiO2@CS-VANCO nanocomposites during 24 h, which was selected to examine their antimicrobial effects under in vivo conditions. The nisin was grafted onto the nanocomposites at around 73.2–87.2%. All the compounds resulted in a marked reduction in the bacterial burden (P-value < 0.05).ConclusionThe vancomycin-functionalized nanocomposites exhibited to be more efficient in eradicating the bacterial cells both in vitro and in vivo. These findings introduce a novel bacteriocin–metallic nanocomposite that can suppress the normal bacterial function on demand for the treatment of MRSA skin infections.

Design and characterization of nano sponges loaded vaginal gels of Voriconazole

Objectives: The current inquiry of this research job is to build and analyze a bio adhesive vaginal gel that is packed with Voriconazole Nano sponge for an extended residence duration at the point of infection, resulting in a positive drug release profile. Methods: Nano sponges were created using a solvent evaporation process in varied Voriconazole to β-cyclodextrin ratios. Zeta possibility, polydispersity, size of particles analysis, capture efficiency, and surface morphology of Nao sponges are all determined using scanning microscopes with electrons (SEM). FTIR and DSC investigations were used to determine drug excipient compatibility. Carbopol/Hypromellose/Sodium Carboxymethyl cellulose/HPC has been used to make the bio adhesive gel, while both propyl paraben and a methyl para were employed as antioxidants. Triethanolamine, also was used to regulate the pH, resulting in a transparent gel. The gel base has been incorporated with the improved Voriconazole Nano sponge mixture. The pH, viscosity, spread ability, extrudability, and medication content of Nano sponge in mixes of gels were all investigated. The gel's in vivo diffusion has been examined on goat vaginal mucosal. Cellophane membranes was used in an artificial drug release examination. Results: The improved generation of IDLNS12 Nano sponge (drug-polymer ratio 1:1) demonstrated 91.56% entrapment efficiency. The average particle diameter of all formulations was less than 310 nm. The SEM photographs revealed smooth and spherical particles. INSG4 (Carpool and HPC) gel formulation had a viscosity value of 4529 cps at 2-10 RPM, a gel strength of 92.65N load, and an expansion speed of 37.24 g.cm/seconds. At 12.0 minutes, INSG4 achieved 99.98% drug release. And a mucous adhesive time of in excess of 12 hours. Conclusion: These results suggest that Voriconazole-loaded β-cyclodextrin Nano sponge in mucous adhesive gel might be used for managing infections of vagina perpetually.

Solubility and Taste Masked Behaviour of Cyclodextrin Molecular Inclusion Complex of Artemether

Artemether by forming a complex with β-cyclodextrine (βCD) is used to improve solubility and taste masked by the kneading method. Artemether with β-cyclodextrine complex prepared with βCD in a drug-polymer ratio 1:1 gave complete taste masking with the satisfactory result obtained in term of in-vivo and in-vitro evaluation. The standard calibration curve of Artemether shows a slope of 0.0154 and a correlation coefficient of 0.9992. Compatibility studies show that drugs are compatible with polymers. Solubility studies show that the solubility of drug are increased in Phosphate buffer 6.8 by successfully forming a complex with βCD. In-vitro dissolution results showed that a maximum of 97.05% of Artemether, drug release less than 15 minutes in formulation. The solubility of Artemether in saliva (PH 6.8) is 0.00735 mg/mL, After complex forming with β-cyclodextrin the solubility of (Artemether complex) is 0.124 mg/mL. In-vitro drug release investigation, taste masking occurs when the amount of drug substance in the dissolve medium is either not identified or is below the threshold for recognizing its flavor in the early time points (between 0 and 5 minutes). Taste masking ( Taste perception test) 11 volunteers were selected for this test, results show that complex is taste masked. Artemether with βCD complex is a hopeful method to augment the solubility, dissolution and taste masking of the drug.

Solubility and Taste Masked Behaviour of Cyclodextrin Molecular Inclusion Complex of Lumefantrin

Lumefantrine is an antimalarial drugs used especially for pediatric persons. β-Cyclodextrine is used to improve the taste of lumefantrine by forming complexes with them by the solvent evaporation method, respectively. β-Cyclodextrine prevent the release of drug in the saliva. Lumefantrine is a bitter drug. So masking of bitter taste in the formulation is a prerequisite as it improves the compliance of the patient and product value. Lumefantrine with β-cyclodextrin in a drug-polymer ratio 1:1 gave complete taste masking with a satisfactory result obtained in term of in-vivo and in-vitro evaluation visual inspection revealed that lumefantrine was yellow-crystalline. The melting point of lumefantrine was found to be 127℃, respectively. The standard calibration curve of Lumefantrine shows a slope 0.0108 and a correlation coefficient of 0.9997. Compatibility studies show that drugs are compatible with polymers. Solubility study show that the solubility of both drugs are increased in phosphate buffer 6.8 by successfully forming a complex with β-cyclodextrin. The solubility of lumefantrine in saliva (pH 6.8) is 0.408 mg/mL, after complex forming with β-cyclodextrine the solubility of (Lumefantrine complex) is 0.526 mg/mL. In an in-vitro drug release investigation, taste masking occurs when the amount of drug substance in dissolved media is either below the detection threshold for recognizing its taste or is undetectable in the early time points (between 0 and 5 minutes). Taste masking (Taste perception test) 11 volunteers are selected for this test, results show that complex is taste masked successfully. Lumefantrine with β-Cyclodextrine complex is a hopeful approach to enhance solubility, dissolution and drug taste.

Evaluation of Insulin Loaded Microspheres for Oral Delivery

Microsphere-based colon-specific medication delivery devices should improve bioactive chemical administration and residence periods. In the first step, insulin microspheres were made using Eudragit RL 100 and L-100 by quasi-emulsion solvent diffusion. Microspheres were made since prior research showed that colon tissue macrophages could take up drug carrier systems with a molecular weight of 956 m or less. The uptake process allows accurate medication delivery to the specified site. Microspheres’ longer residence time than conventional drug delivery methods may allow dosage reduction and therapeutic efficacy. Because microspheres are permeable, they may be compacted and used to make stronger tablets. Thus, the CPDRS1 formulation performs well, enabling insulin delivery via an anti-diabetic microsphere. Drug-polymer ratio affects microsphere size and form. Variations in emulsifying agent amounts affect microsphere sizes and manufacturing yield. Using appropriate polymer and emulsification agent concentrations improves insulin-loaded Eudrajit L microsphere (Eudrajit RL) formulation and manufacturing yield