Cumulative Percentage Drug Release Research Articles

Formulation and Characterization of Carvedilol In situ Gels for Oral Delivery-In vitro and In vivo Pharmacokinetic Studies

The purpose of the study is to develop floating in situ gelling oral delivery system of carvedilol. Before formulating into in situ gels, carvedilol was first made into solid dispersions to enhance its solubility. The solvent evaporation method was employed for making solid dispersions. Drug content, solubility, dissolution, SEM, DSC, and XRD studies were done for solid dispersions. In situ gel formulations were prepared using the optimized solid dispersion formulation. Sodium alginate and HPMC K100M were used as gelling agent and viscosity enhancing agent respectively. In vitro characterizations like gelling capacity, floating time, drug content, viscosity, and % cumulative drug release studies were done. In vivo pharmacokinetic parameters like Cmax, Tmax, half-life, AUC, AUMC, and MRT were studied. FTIR studies ruled out any drug-excipient interactions. The drug release pattern showed a burst effect in the first 30 minutes then followed by a steady release for 12 hours. Stability data indicated that the formulation remained stable with no significant changes in drug content, viscosity, and percent cumulative drug release upon storage. In vivo pharmacokinetic study results were found to be satisfactory. A stable, sustained release, liquid oral floating in-situ gelling systems of carvedilol were successfully formulated and evaluated.

Solubility Enhancement of Ebastine by Formulating Microemulsion Using D-Optimal Mixture Design: Optimization and Characterization.

Ebastine, a histamine H1 antagonist, nonsedating, belonging to BCS class II is used in the treatment of allergic rhinitis and chronic idiopathic urticaria. The current study was intended in augmenting the aqueous solubility and dissolution rate of ebastine, by formulating a microemulsion system using oleic acid, Transcutol® HP, and Tween®80 as oily phase, cosurfactant, and surfactant, respectively, by the phase titration method. A custom mixture design with optimality D was used to design the formulation by using the Design Expert® Software (Version 11; Stat-Ease, Inc., Minneapolis, MN, USA). Optimization of formulation was performed using the numerical optimization technique, where optimization is based upon the desirability. The optimized formulation was evaluated for transmittance, viscosity, globule size, polydispersity index, zeta potential, drug content, morphological studies, and in vitro studies. The optimized formulation displayed percent cumulative drug release, ranging from 82.9% to 90.6% obtained after dissolution studies and the percent cumulative drug release after diffusion studies ranged from 83.3% to 100%. The in vitro release data were subjected to kinetic treatment. The zero-order and first-order plots were linear and showed the highest values for R2, which indicated mixed-order release. The Higuchi plot was linear, indicating diffusion as the mechanism of release. From Peppas plot, it was further confirmed that the release for dissolution studies was anomalous and for diffusion studies it was zero order. Thus, the studies concluded that the microemulsion technique is a very good approach for enhancing the solubility and dissolution rate of the BCS class II drug ebastine.

Study on the formulation of transdermal patches of zolpidem tartrate therapy

Getting a controlled and sustained dose of Zolpidem tartrate therapy for the treatment of anxiety disorders was the purpose of the current study. The technique of film casting was utilised in the preparation of the matrix type of transdermal drug delivery. In order to characterise and evaluate the formulations, various parameters such as in vitro drug release and skin permeation studies were conducted. The effect of varying ratios of matrix-forming polymer, specifically Eudragit RL 100 and Eudragit RS100, combined with PVP K 30 was investigated in terms of its influence on in vitro drug release. According to the findings, the percentage of cumulative drug release after 48 hours for each of the different formulations ranged anywhere from 66 to 81 percent. The values that corresponded to the cumulative amount of drug permeation ranged anywhere from sixty to eighty percent. This innovative method of administering the drug via the skin results in a greater amount of the drug's effects being maintained over time.

STUDIES ON FORMULATION AND EVALUATION OF LIPOSOME FOR CUTANEOUS LEISHMANIASIS

Aim of present study was to design liposome for allopurinol delivery against cutaneous leishmaniasis (CL). Leishmaniasis is disease caused by pathogenic protozoan parasites of the genus Leishmania. The disease is complex and untreated cases of leishmaniasis may result to chronic form such as mucosal leishmaniasis. There are several therapeutics available to treat CL, however, in recent time allopurinol has been used to tackle the chronic cases. The conventional formulations of allopurinol remain associated with several limitations both pharmacokinetic and pharmacodynamic. In this study, nanodesign liposome has been used to enhance pharmacokinetic and pharmacodynamic parameters. The liposomes were prepared by dried thin film hydration technique using a rotary evaporator with drug and carrier (soybean lecithin). The prepared liposomes formulations were evaluated for physical and chemical characteristics like average vesicle size, shape, zeta potential, % free drug, assay and stability studies. This developed liposomal drug delivery system was also evaluated for in-vitro drug release studies by pH 7.4 phosphate buffer using membrane diffusion method. The cumulative percentage of drug release was reported highest in the LF4 i.e. 98.08±1.54. Additionally, ex vivo studies have shown that allopurinol loaded into liposome has higher permeation (2.68µg/cm2 ) compared to allopurinol alone. These finding demonstrate liposome based allopurinol based drug delivery is effective compared to conventional formations.

Formulation Development and Evaluation of Floating Tablets of Zolmitriptan

Zolmitriptan is the antimigraine agent widely used for the treatment of the migraine. It shows the half-life of 2.5 – 3 h which indicate the frequent dosing to achieve proper pharmacological action of the drug. Gastro Retentive Drug Delivery System (GRDDS) is a common approach to decrease the dosing frequency and increase patient compliance, and delivery of drug through such an approach of floating tablet formulation will meet the requirement. This system showed substantial effect on the drug release through floating and swelling properties. The tablets were formulated by using direct compression technique along with hydrophilic polymers and gas generating system. In the preliminary trials, we observed that the tablets were within pharmacopeial limit. % Drug release of the formulations (F1 – F9) was studied up to 6 h and it was found from 52 to 91 %. The cumulative percentage drug release was inversely proportional to polymer concentrations of HPMC K100 M and PVP K 30. The batches follow Higuchi model of drug release which involves the diffusion mechanism. In-vitro dissolution studies showed good percent drug release, which is in accordance with robinson-errikson equation. Good buoyancy for additional 6 h, trailed by the diffusion.

Preparation and Evaluation of Sustained Release Microbeads Containing Ibuprofen

The current study was carried out in order to prepare sustain release multiparticulate drug delivery system of Ibuprofen which is also known as 2-(4-isobutylphenyl) propionic acid. From the drug excipient study it was found that the drug and polymer were compatible with each other and there was no disappearance, new formation of peaks on the FTIR study. From the DSC study it was seen that there was no change in the melting point of drug when mixed with the polymers. The method applied was Ionotropic gelation. The Microbeads were prepared by employing sodium alginate as a coating agent with HPMC as release retardant and calcium chloride as a cross linking agent. The prepared microbeads were evaluated for various parameters such as micromertics, loose surface crystal study, percentage yield, percent cumulative drug release and surface morphology. From the various evaluated parameters it was revealed that the prepared microbeads were having a good flow property. The percentage yield was found to be in the range of 65.23% - 79.45%, the drug release was found to be in the range of 4.96% - 96.08%. The batch of B7 was the optimized one as it contain higher amount of drug content and shows better amount of drug release then the other batches. The surface morphology study revealed that the optimized formulation was having small cracks or fractures on the surface. From the study we can conclude that this method can be employed for preparing microbeads of Ibuprofen without any difficulty and this formulation can utilized for reducing the dose frequency of Ibuprofen which will not hinder the GIT.

Development and evaluation of raloxifene hydrochloride-loaded subdermal implants using hot-melt extrusion technology

Implantable drug delivery systems are known to provide great patient compliance and allow for controlled delivery of drugs over a prolonged period of time. This study aimed to prepare novel polycaprolactone/polyethylene glycol-based raloxifene hydrochloride subdermal solid cylindrical implants using a single-step hot-melt extrusion (HME) continuous process, for the provision of a sustained and prolonged release of RX-HCl as a cornerstone and alternative treatment and prevention option of osteoporosis, most especially post-menopausal osteoporosis, and invasive breast cancer, while providing better clinical outcomes by circumventing clinical and biopharmaceutical hurdles like first-pass metabolism and patient non-adherence and incompliance associated with the oral dosage forms of raloxifene hydrochloride. The 11-mm co-rotating twin-screw extruder was used to prepare the implants. The prepared cylindrical-shaped solid implants with dimensions of 10 mm (length) by 2 mm (diameter) were characterized by DSC, PXRD, FTIR, SEM, and in vitro dissolution analysis. Based on the physicochemical characterization of the prepared implants, the HME fabrication technology and optimized process parameters were determined to be acceptable and suitable. The prepared implants showed no obvious burst release and no significant amounts of drug on the surface of the implants. F-1, F-2, and F-3 implant batches showed a maximum cumulative percent drug release of 82.9%, 42.2%, and 20.6%, respectively, in a period of 30 days, and 100% drug release would be expected in a period of about 40 days (F-1), 72 days (F-2), and up to 150 days (F-3) by simple extrapolation. Interestingly, implant batches with a low drug load exhibited a relatively faster and higher rate of release of the drug compared to implant batches with high drug loading. In the present study, a single-step HME process was successfully used to fabricate RX-HCl-loaded subdermal implants, that could potentially be used as a cornerstone regimen in the treatment and prevention of osteoporosis, most especially post-menopausal osteoporosis, by providing release of RX-HCl over a long time period, and avoiding the clinical inconveniences and possible patient incompliance caused by daily administration of the drug.

Developed meloxicam loaded microparticles for colon targeted delivery: Statistical optimization, physicochemical characterization, and in-vivo toxicity study.

The study aimed to fabricate and evaluate Meloxicam (MLX) loaded Hydroxypropyl Methylcellulose (HPMC) microparticles for colon targeting because MLX is a potent analgesic used in the treatment of pain and inflammation associated with colorectal cancer (CRC). Nevertheless, its efficiency is limited by poor solubility and gastrointestinal tracts (GIT) associated side effects. Seventeen formulations of MLX loaded HPMC microparticles were fabricated by the oil-in-oil (O/O)/ emulsion solvent evaporation (ESE) technique. A 3-factor, 3-level Box Behnken (BBD) statistical design was used to estimate the combined effects of the independent variables on the dependent variables (responses), such as the percent yield (R1), the entrapment efficiency (EE) (R2), mean particle size (R3) and in vitro percentage of cumulative drug release (R4). For physicochemical characterization FTIR, XRD, DSC, and SEM analyses were performed. Biocompatibility and non-toxicity were confirmed by in-vivo acute oral toxicity determination. The percentage yield and EE were 65.75-90.71%, and 70.62-88.37%, respectively. However, the mean particle size was 62.89-284.55 μm, and the in vitro cumulative drug release percentage was 74.25-92.64% for 24 hours. FTIR analysis showed that the composition of the particles was completely compatible, while XRD analysis confirmed the crystalline nature of the pure drug and its transition into an amorphous state after formulation. DSC analysis revealed the thermal stability of the formulations. The SEM analysis showed dense spherical particles. The toxicity study in albino rabbits showed no toxicity and was found biocompatible. The histopathological evaluation showed no signs of altered patterns. Results of this study highlighted a standard colonic drug delivery system with the ability to improve patient adherence and reduce GIT drug-associated side effects in CRC treatment.

Formulation and characterization of nimodipine in situ gels for oral delivery

To formulate and evaluate Nimodipine floating in situ gels for oral delivery in order to enhance its residence time and to overcome the inherent drawbacks associated with conventional oral formulations like tablets and capsules. As Nimodipine is a BCS Class II drug, first Nimodipine solid dispersions were made to enhance its solubility. Solvent evaporation method was employed for this. Then in situ gel formulations were prepared using the optimized solid dispersion formulations. Sodium alginate and HPMC K100M were used as gelling agent and viscosifying agent respectively. In vitro characterization like gelling capacity, floating time, drug content, viscosity, % cumulative drug release studies were performed. In vivo pharmacokinetic parameters were studied. Infrared spectroscopy ruled out drug-excipient interactions. The release pattern showed a burst effect in the first 30 minutes followed by a moderate steady release for 12 hours. Stability testing indicated that the formulation remained stable with no significant changes in percent cumulative drug release and viscosity. In vivo pharmacokinetic study results were satisfactory. A promising, stable, sustained release, liquid oral floating in-situ gelling systems of Nimodipine were successfully developed and evaluated. Oral in situ gels could be good alternative for geriatric and pediatric population who have trouble swallowing solid medications.

QbD-Enabled Systematic Development of Ileo-Colonic Targeted Novel Mucoadhesive Microspheres of Flurbiprofen.

Flurbiprofen (FLBP), used in the treatment of ulcerative colitis, has a short biological half-life. Frequent intake of FLBP may lead to some serious gastric complications, which makes FLBP an ideal candidate for sustained release preparation to the Ileo-colonic region of the gastrointestinal tract (GIT). The objective of this study was to investigate the potential of Eudragit coated chitosan microspheres in delivering Flurbiprofen in a sustained manner to the Ileo-colonic region of the GIT for treatment of ulcerative colitis. In the present study, mucoadhesive chitosan microspheres were prepared using the emulsion solvent evaporation method by varying different process parameters. Optimized chitosan microspheres were coated with Eudragit L-100 and Eudragit S-100. A 32 full factorial design was applied for optimization. The effect of independent variables (Eudragit L-100 to Eudragit S-100 ratio and stirring speed) on dependent variable i.e. percentage cumulative drug release (%CDR) at 3 h and 24 h was evaluated. The optimized batch was evaluated by FT-IR, DSC study, XRD study and SEM analysis. Discrete spherical shape chitosan microspheres with entrapment efficiency of up to 95.4% were obtained and selected for coating. Chitosan microspheres were coated successfully with different ratios of Eudragit L-100 to Eudragit S-100. The release profile of the optimized batch matches with the desired release profile. FLBP was found to be stable and molecularly dispersed in the polymer matrix. Taken together it can be concluded that prepared microspheres may be considered as a suitable for delivering FLBP to the Ileo-colonic region of the GIT in the treatment of ulcerative colitis.

DEVELOPMENT OF NANO BASED FILM FORMING GEL FOR PROLONGED DERMAL DELIVERY OF LULICONAZOLE

Objective: Luliconazole (LZL) has low aqueous solubility that limits its dermal bioavailability and acts as a barrier to topical delivery. The conventional topical formulations have a limited ability to retain the drug over the skin for a prolonged period. The main objective of the study was to formulate and characterize LZL loaded ethyl cellulose (EC) nanoparticles and formulate them as a film-forming gel (FFG) for prolonged delivery in fungal skin infections.Methods: The solvent evaporation technique was used for the preparation of nanoparticles of LZL by using EC as a polymer. The prepared nanoparticles were evaluated for physical appearance, production yield, entrapment efficiency, drug content, particle size, zeta potential, Polydispersity index (PDI), and in vitro drug release. Then the nanoparticles were incorporated into FFG formulation by using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA) as the gelling agent. The prepared FFG was evaluated for pH, Viscosity, Spreadability, in vitro drug release studies, in vitro antifungal studies, and release kinetic studies.Results: The optimized nanoparticle formulation F5 having drug to polymer ratio of 1:2 showed satisfactory production yield (86.32%), entrapment efficiency (83.36%), drug content (42.86), particle size (125.3), and 93.72% of in vitro drug release after 24 h (h). The optimized FFG formulation FFG4 showed the shortest film-forming time of 5.06 min (min), percentage Cumulative drug release of 92.18% after 24 h, and had promising in vitro antifungal activity.Conclusion: The prepared FFG could be used with promising potential for fungal infection of the skin.

Formulation and Evaluation of Colon Targeted Drug Delivery System

Purpose:The objective of the present study was to develop colon targeted drug delivery system of Metronidazole using guar gum as the carrier.Methods:Matrix tablets containing various proportions of guar gum were prepared by direct compression technique. Rapidly disintegrating Metronidazole core tablets were prepared and compression coated with guar gum and 20% of microcrystalline cellulose. The tablets were evaluated for hardness, thickness, drug uniformity and subjected to in vitro drug release studies under conditions mimicking mouth to colon transit. Results and Conclusions: The FTIR study indicates no possible interaction between Metronidazole and carriers. The tablets were found within the permissible limits for various physiological parameters. In vitro drug release studies in pH 6.8 phosphate buffer solution containing rat cecal contents have demonstrated the susceptibility of guar gum to the colonic bacterial enzyme action with consequent drug release. The pretreatment of rats orally with 1 ml of 2% w/v aqueous dispersion of guar gum for 7 d induced enzyme specifically acting on guar gum thereby increasing drug release. Dissolution studies were performed in 0.1N HCl for 2 h, in pH 7.4 buffer for 3 h and pH 6.8 up to 24 h. The cumulative percentage of drug release of Metronidazole after 24 h in pH 6.8 phosphatebuffers was found to be 98.51±0.02, 86.69±0.02, 84.55±0.04, 39.31±0.02, 24.60±0.02, 18.85±0.02 for formulation F1, F2, F3, F4, F5 and F6. It can be concluded that formulation F1 is considered a potential formulation for targeting the drug to the colon. The results showed that guar gum protects the drug from being release completely in the physiological environment of stomach and small intestine.©2022iGlobal Research and PublishingFoundation. All rights reserved.

Response Surface Methodology-Based In Vitro And In Vivo Evaluation Of Nsaid-Loaded Eudragit Microspheres

This study targets on the development and characterization of extended-release microspheres loaded with the nonsteroidal anti-inflammatory drug (NSAID) Aceclofenac, using the Eudragit RS-100 polymer. To use a single emulsion [oil-in-oil] solvents evaporation technique, the microspheres were created, with the impact of three independent variables (poly vinyl acetate, polymer, and stirring speed) evaluated using Design-Expert® Software and response surface methodology. The dependent variables chosen were encapsulation efficiency, vesicle size, and cumulative drug release. Many methods were used to analyse the microspheres, including X-ray powder diffraction, infrared spectroscopy using the Fourier transform, particle size measurement, and field emissions scanning electron microscopy. The safety and effectiveness of the formulation were also confirmed by in vitro and in vivo drug release experiments. The results showed that the microspheres had a spherical shape with a non-porous surface morphology and a mean particle size of 45±1.23µm. The percentage of encapsulation efficiency ranged from 56±0.82 to 82±0.65, and the percent cumulative drug release ranged from 57±5.6 to 74±4.6. The Eudragit RS-100 polymer demonstrated a sustained drug release profile of up to 14 hours, with higher and longer-lasting anti-inflammatory activity than pure Aceclofenac. The microspheres showed potential in improving patient compliance with minimal or no adverse effects, and their physical appearance and drug content were not affected by accelerated stability testing. Overall, Eudragit RS-100 proved to be an effective sustained-release carrier for developing Aceclofenac-loaded microspheres that enhance efficacy with minimal gastrointestinal side effects during long-term use.

Neoteric Approach of Fluoxetine Laden Orodispersible Film for Non-compliant Pediatric Patients of Selective Mutism and Obsessive-compulsive Disorder.

The objective of this research was to fabricate, characterize, and optimize fluoxetine laden orodispersible film (ODF), in enhancing dosage forms options for the pediatric population suffering from incapacitating psychotic disorders of selective mutism and obsessive-compulsive disorder, which will be ultimately beneficial in enhancing compliance factor and the quality of pharmacotherapy. Solvent casting technique was used to formulate the ODF formed by natural hydrophilic polymers matrix of hydroxypropyl methylcellulose E15 and pullulan. Propylene glycol as plasticizing agent imparted satisfactory tenacity and flexibility to ODFs. Fourier transform infrared spectroscopy studies were performed to investigate any potential compatibility, and the results revealed no potential interaction between fluoxetine and excipients. Developed ODFs were evaluated for physicochemical properties, content uniformity, in vitro disintegration time, and in vitro dissolution time studies. Results: The experimental data. The experimental data suggested that different polymer concentrations had a complex effect on content uniformity, in vitro disintegration time, and cumulative percentage drug release from the ODFs. TF7 was the most optimized formulation with a disintegration time of 10.66 sec and 99.37% drug release within 3 min. Additionally, the most optimized fluoxetine ODF was submitted to a Universal Testing Machine for tensile strength and percentage elongation determination. It was also further evaluated by thermogravimetric analysis, scanning electron microscopy and X-ray diffraction. Fluoxetine ODFs of good pharmaceutical quality can be prepared on a small scale. Therefore, the perspective of using fluoxetine ODFs for individualized pharmacotherapy to ameliorate the compliance issues in selective mutism and OCD pediatric patients can be considered.

Development and Characterization of Repaglinide Loaded Floating Microparticles

Sustained release drug delivery has been successfully achieved using microparticles made from natural or synthetic polymers. The aim of this study is to develop and test floating microparticles of Repaglinide in order to improve drug bioavailability by extending gastric residence time. Repaglinide, an oral hypoglycemic, is a lipophilic drug that is rapidly absorbed from the stomach and eliminated with a half-life of just 1 h, so suitable to be formulated as floating drug delivery system for sustained release.Repaglinide floating microparticles were developed using an ionotropic gelation method that included calcium chloride as a cross-linking agent, sodium alginate, and different concentrations of hydroxypropyl methylcellulose (HPMC), ethyl cellulose (EC), and sodium bicarbonate (NaHCO3). A three factor, three-level Box-Behnken design was used to study the effect of independent variables on dependent variables. In the formulation of microparticles, the amount of hydroxypropyl methylcellulose (X1), ethyl cellulose (X2), and sodium bicarbonate (X3) were three independent variables, while percentage buoyancy (Y1) and percentage drug release at 10 h (Y2) were dependent variables. Micromeritic properties, percent yield, percent drug entrapment performance, surface morphology, percent buoyancy, in-vitro drug release, and drug excipient compatibility were all assessed in the formulations.FTIR studies revealed no interaction between the drug and the excipients.SEM for surface morphology studies revealed that their surface is spherical and smooth. The mean particle size of formulations was found to be between 415- 689 µm, the drug entrapment efficiency was found to be between 44.65% - 76.55% and percent buoyancy was noted to be between 63%- 78.33%. The results revealed that entrapment efficiency increased as polymer concentration was increased. The cumulative percent drug release after 10 h was noted to be between 76.87- 88.12%. Percent drug release decreased as polymers concentration was increased. The buoyancy was increased with increasing concentration of sodium bicarbonate. The developed microparticles could successfully retard the release of the drug.

Formulation & charecterizaion of anti-microbial property of herbal oral in-situ gel

Optimisation, formulation, and characterisation of an oral in situ gel containing clove oil are the focus of the current study. When it came to cross-linking and viscosifying agents, sodium alginate was utilized. The floating agent was sodium bicarbonate. pH were determined to be 7.2 in preformulation experiments. No differences were found between medication and polymers in FTIR spectrums during compatibility testing. There was good pourability in all of the formulas. It took 30 s to float, and it took a total of >12 h to float. Drugs were released from the formulation at a rate of 80–95 percent over 5–6 h during in vitro drug release tests. It was discovered that the concentration of sodium alginate and HPMC had a substantial impact on floating delay, gelling capacity, and cumulative percentage drug release in these experiments. When we tested clove oil (Eugenol) as an antibacterial, we discovered that it demonstrated good zone of inhibition against diverse microbial strains (Staphylococcus aureus and Escherichia coli).

Utilization of Gelling Polymer to Formulate Nanoparticles Loaded with Epalrestat-Cyclodextrin Inclusion Complex: Formulation, Characterization, In-Silico Modelling and In-Vivo Toxicity Evaluation.

Epalrestat (EPL) is an aldose reductase inhibitor with poor aqueous solubility that affects its therapeutic efficacy. The research study was designed to prepare epalrestat-cyclodextrins (EPL-CDs) inclusion complexes to enhance the aqueous solubility by using beta-cyclodextrin (β-CD) and sulfobutyl ether₇ β-CD (SBE7 β-CD). Furthermore, polymeric nanoparticles (PNPs) of EPL-CDs were developed using chitosan (CS) and sodium tripolyphosphate (sTPP). The EPL-CDs complexed formulations were then loaded into chitosan nanoparticles (CS NPs) and further characterized for different physico-chemical properties, thermal stability, drug-excipient compatibility and acute oral toxicity studies. In-silico molecular docking of cross-linker with SBE7 β-CD was also carried out to determine the binding site of the CDs with the cross-linker. The sizes of the prepared NPs were laid in the range of 241.5–348.4 nm, with polydispersity index (PDI) ranging from 0.302–0.578. The surface morphology of the NPs was found to be non-porous, smooth, and spherical. The cumulative percentage of drug release from EPL-CDs loaded CS NPs was found to be higher (75–88%) than that of the pure drug (25%). Acute oral toxicity on animal models showed a biochemical, histological profile with no harmful impact at the cellular level. It is concluded that epalrestat-cyclodextrin chitosan nanoparticles (EPL-CDs-CS NPs) with improved solubility are safe for oral administration since no toxicity was reported on vital organs in rabbits.

Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation

Background & ObjectivesLow penetration efficiency and retention time are the main therapeutic concerns that make it difficult for most of the drugs to be delivered to the intraocular tissues. These challenging issues are often related to those drugs, which have low or poor solubility and low permeability. The goal of this study was designed to develop nanostructured lipid carriers (NLCs) loaded with itraconazole (ITZ) with the objective of enhancing topical ocular permeation and thereby improving clinical efficacy. Materials and MethodsITZ-loaded NLCs were fabricated by a high-speed homogenization technique using surfactant (Poloxamer 407), and lipids (stearic acid and oleic acid). Optimization of formulations was performed by 3 level factorial design and the selected formulation (F6) was evaluated by differential scanning calorimetry and transmission electron microscopy. Antifungal activity was assessed by measuring the zone of inhibition and irritation potential using the HET-CAM test. ResultsThe independent variables (lipid ratio-X1 and percentage of emulsifier-X2) have a positive impact on percentage entrapment efficiency (Y2) and percentage release (Y3) but have a negative impact on particle size (Y1). Based on the better entrapment efficiency (94.65%), optimum particle size (150.67 nm), and percentage cumulative drug release (68.67%), batch F6 was selected for further evaluation. Electron microscopic images revealed that the prepared particles are spherical and have nano size. Antifungal studies demonstrated enhancement in the zone of inhibition by formulation F6 as compared to a commercial eye drop. The non-irritancy of optimized formulation (F6) was confirmed with a zero score. Interpretation & ConclusionIn summary, the optimized NLCs seem to be a potent carrier for the effective delivery of itraconazole in ocular therapy.

DEVELOPMENT AND EVALUATION OF MOUTH DISSOLVING ANTIINFLAMMATORY TABLET CONTAINING FENOPROFEN

Fenoprofen belongs to Biopharmaceutical Classification System (BCS) class II drugs which are poorly soluble in water. The objective of present research work was to prepare fast dissolving tablets of fenoprofen using varying concentrations of three different sublimating agents to improve the dissolution rate. Seven formulations were prepared containing different concentrations of camphor, ammonium bicarbonate and thymol as sublimating agent along with primogel as a superdisintegrant. Tablets were manufactured by direct compression method. The prepared tablets were evaluated for pre-compression and post-compression parameters result, for all formulations result was within official limits. DSC studies revealed that there were no interactions between the drug and the excipients used. From in vitro drug release studies the dissolution studies, cumulative percentage of drug release versus time was evaluated. It also reflects that the formulations F4 and F15 containing 45 mg and 67.5 mg of thymol respectively showed fast drug release of 100.00% and 99.56 % respectively in 30 minutes as compared with formulations containing other sublimating agents. Among all the formulations, F6 and F7 tablets showed complete drug release within 30 minutes and rapid dissolution.

Enhancement of dissolution profile of poorly aqueous soluble atorvastatin calcium by binary and ternary solid dispersion techniques

Atorvastatin calcium (ATV) is an HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase inhibitor commonly known as a cholesterol-lowering agent. As a poorly water-soluble drug its absolute bioavailability is very low. To increase the water solubility as well as oral bioavailability, different hydrophilic carriers were used in different ratios (1:0.5, 1:1 and 1:2) to prepare reproducible binary and ternary solid dispersion formulations of ATV by simple physical mixing (PM) and fusion or melting technique. In vitro dissolution studies results revealed that in all cases, the cumulative percent drug release from ATV ternary SD formulations were greater than binary formulations, some marketed products and pure ATV powder. The order of the carriers in enhancing the drug release was found as kollidon 90F > pregelatinized starch > lutrol> kollidon 12F (99.1%, 98.8%, 96% and 95% respectively) for ternary SD formulations whereas pure ATV powder and marketed products showed cumulative percentage release 70.8%, 68.9% (B1) and 73.1% (B2), respectively. The best-out performed ternary SD formulation ATV:Kollidon 90 F (1:2) were further characterized using FT-IR and SEM. SEM analyses indicated conversion of crystal drug to amorphous form and FT-IR data suggested that little or no interaction between the drug and polymer. Bangladesh J. Sci. Ind. Res.56(3), 165-176, 2021