Hydroxyl Propyl Methyl Cellulose Research Articles

Formulation and Antimicrobial studies of Microencapsulated Musanga cecropioides Stem Bark Extract

Microencapsulation is the process of coating small droplets of liquid or solid materials with a continuous film of polymeric substances. The aim of the research was to formulate microparticles of Musanga cecropioides stem bark extract. The dried, powdered stem bark of Musanga cecropioides was extracted by maceration. The aqueous extract was microencapsulated using polymers such as alginate, pectin and hydroxylpropyl methylcellulose acetate succinate (HPMCAS) by counter-ion coacervation method using an electrostatic droplet generator. The formulated microcapsules were evaluated for flow properties, particle size, drug content, antimicrobial activity and in vitro release kinetics in simulated gastric and intestinal fluids. The microparticles were subjected to stability tests under different temperature (45°C, 25°C and 8°C) and relative humidity (100% RH, 78% RH and 0% RH) conditions for a period of three (3) months. The mean particle size of the microcapsules decreased with increasing applied voltage of the electrostatic generator. Particle size range for the batches of formulated microparticles was 68.20-223.84µm. The percentage entrapment efficiency of the batches of microparticles ranged from 80.26-86.58%. The microparticles lost a significant percent of its drug content after storage at different temperature and relative humidity conditions. The formulated microparticles and crude extract possess significant antibacterial action against both gram positive and negative bacteria as well as antifungal effect against C. albicans. Microparticles of M. cecropioides extract were formulated by counter-ion coacervation method using an electrostatic droplet generator which conferred advantages of sustained drug release, reduced frequency of dosing, masked unpalatable taste, improved stability and enhanced patient acceptance on the crude extract.

Formulation and validation of Candesartan cilexetil-loaded nanosuspension to enhance solubility

The following research aimed to enhance solubility by loading candesartan cilexetil into nanosuspension. Candesartan cilexetil-loaded nanosuspension was prepared with the aid of Design-Expert® software. A technique of solvent evaporation was employed to produce nanosuspensions from hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl pyrrolidone (PVP K-30), and poloxamer (PXM 188). The optimised nanosuspensions’ particle size and polydispersity index (PDI) were 64.65 nm and 0.059, respectively. The entrapment efficacy (EE %) and drug loading (DL %) were 86.75 and 10.17%, respectively. The atomic force microscopy (AFM) revealed spherical and smooth nanoparticles. The Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) revealed pure, crystalline and conjugated drugs inside the nanosuspension. The release study confirmed 90% release within 10 min. No significant changes in particle sizes over three months were found, indicating stable nanoparticles. Saturated solubility of the candesartan cilexetil powder and loaded nanosuspension was 63.3 ± 6 and 344.7 ± 16 µg.ml-1, respectively, revealing more than five times increase in solubility. Candesartan cilexetil-loaded nanosuspensions were successfully prepared using different combinations of PVP K-30, HPMC E-5 and PXM 188 in various concentrations. Solubility was enhanced by loading the payload into nanosuspensions.

Formulation and Evaluation of Naproxen Sodium Transdermal Patches Using Natural Polymer

Natural polymer from flaxseed Linum usitatissimum was used in this study to develop a matrix-dispersion type transdermal Naproxen sodium medication delivery system. Flaxseed mucilage and hydroxyl propyl methyl cellulose were used to make transdermal patches of naproxen sodium. Transdermal patches were made using flaxseed mucilage, whichwas adopted and tested for its impact on patch quality. The solubility, melting point, and partition coefficient of the medication have been determined as preliminary evaluation metrics. Using Franz diffusion cells, the produced patcheswere assessed in vitro for in vitro drug release, folding durability, thickness, and weight fluctuation of the patches. For FTIR and DSC, and a stability analysis, the improved formulation was used. Data from FTIR and DSC demonstrated that the medication and excipient had no significant interaction. Keywords: naproxen sodium, flaxseed mucilage, solvent casting method, folding endurance, Franz diffusion cell.

Investigating the efficacy of mirtazapine-embedded invasomal gel nanocarriers via I-optimal design for management of atopic dermatitis

The objective of the present study was to optimize a novel invasomal gel (inva-gel) formulation enriched with terpene for upgrading the therapeutic action of anti-depressant mirtazapine on atopic dermatitis as an off-label use. Various factors were studied by I-optimal design to propose an optimized invasome with desirable characteristics. Its incorporation into different hydrogel bases was targeted to suggest a desirable inva-gel formulation, inspect its ex-vivo performance, and conduct in-vivo pre- and post-sacrifice assessments on atopic dermatitis-induced rats. Results revealed positive ethanol action on increasing entrapment efficiency (up to 77.88%) and decreasing size of invasomal vesicles (from 390.30 nm to 190.60 nm). Increased terpene amounts provided more space for mirtazapine incorporation with enhanced solubility and encapsulation inside invasomes. Terpene's molecular weight and lipophilicity significantly affected physicochemical characteristics of invasomes. More cross-linkages would occur by raising gel:liquid invasome ratio (from 0.5:1 to 2.5:1) and using carbopol other than hydroxylpropyl methyl cellulose (HPMC), therefore increasing rheological properties of inva-gels. Synergistic effects of phospholipid, ethanol, limonene, and carbopol to enhance mirtazapine permeation through skin were observed. Throughout the pre-sacrifice assessments, optimized inva-gel demonstrated a significant decrease in dermatitis severity score (from 8.33 to 3.00) and scratching behavior (from 184.32 s to 37.42 s) in disease-induced rats, hence showing favorable skin profile. Concerning the post-sacrifice assessments, optimized inva-gel significantly alleviated inflammation and pruritus symptoms by minimizing epidermal thickening (from 92.32 μm to 50.17 μm), down-regulating various inflammatory mediators, and decreasing infiltration of inflammatory mast cells. Besides, the ear swelling and spleen index values were markedly decreased (from 77.37 mg to 22.76 mg and from 0.56% to 0.35%, respectively). In conclusion, novel anti-depressant mirtazapine-embedded inva-gel displayed successful transdermal drug permeation offering valuable merits in atopic dermatitis management.

Formulation and Evaluation of Gastro Retentive Floating Tablet of Cetirizine Hydrochloride using Linseed Mucilageas Polymer

This study’s objectives were to create and assess gastric-floating controlled release tablets employing flaxseed mucilage as polymer. Linseed mucilage was isolated from Linum usitatissum seeds. Compatibility studies were performed on drug and other excipients. This study employed individual and mixed polymers to manufacture floating CH tablets. The polymers HPMC, MCC, and linseed mucilage were utilized in various ratios. Five distinct formulae were created (F1-F5 by powder a direct compression method. Formulations was tested for various parameters including in-vitro drug release and floating ability. The findings of all evaluation parameters are substantial. With an 8-hour floating time and a medicine release rate of 98.4% at end of the 24 hours, the formulation (F3), including hydroxyl propylmethyl cellulose and Linseed mucilage was shown to be the best. The current study focuses on the formulation of floating tablets using a natural polymer as a binder (Linseed mucilage). However, in-vivo experiments are still needed to establish the efficacy of the manufactured CH floating tablets.

Effects of drying method and oil type on edible polyunsaturated oleogels co-structured by hydroxylpropyl methyl cellulose and xanthan gum

The subtle balance between the interactions of polysaccharide molecules and the interactions of polysaccharide molecules with oil molecules is significantly important for developing polysaccharide-based polyunsaturated oleogels. Here, hydroxylpropyl methyl cellulose and xanthan gum were used to structure edible oleogels via emulsion-template methodology, while the effects of drying methods (hot-air drying (AD) and vacuum-freeze drying (FD)) and oil types (walnut, flaxseed and Moringa seed oil) on the structure, oil binding capacity (OBC), rheological properties, thermal behaviors and stability of oleogels were specially investigated. Compared with AD oleogels, FD oleogels exhibited significantly better OBC, enhanced gelation strength (G' value) and better capacity to holding oil after high temperature processing, which was attributed to the possibly increased oil-polysaccharide interactions. However, the weakened polysaccharide-polysaccharide interactions in FD oleogels failed in providing stronger physical interface or enough rigidity to restrict the migration of oil molecules. Polyunsaturated triacylglycerols in vegetable oils deeply participated in the construction of the network of AD oleogels through weak intermolecular non-covalent interactions, which in turn greatly changed the crystallization and melting behaviors of vegetables oils. In brief, this research may provide useful information for the development of polysaccharide-based polyunsaturated oil oleogels.

Comparison of the effect of hydroxyl propyl methyl cellulose, pectin, and concentrated raisin juice on gluten-free bread based on rice and foxtail millet flour.

The nutritional and technological challenges of gluten-free (GF) bread have increased the need for its modification due to the growing demand for this product, especially from celiac patients. Therefore, the present study aims at evaluating the influence of hydroxyl propyl methyl cellulose (HPMC) at 1% and 2% levels, pectin at 1.5% and 2.5% levels, and concentrated raisin juice (CRJ) at 3% and 4% levels on the dough rheological properties and quality of GF bread based on rice and millet flour. The GF bread prepared with HPMC and incorporating CRJ had higher water absorption, dough development time, and dough stability. In addition, the firmness of GF bread during 24-72 h after baking in the presence of 1% HPMC with 3% and 4% CRJ followed by 2.5% pectin incorporating 3% and 4% CRJ showed a significant decrease compared to the control sample. Further, the color index of GF bread was improved with the addition of HPMC and pectin and the L* index decreased in all GF breads with CRJ. The highest volume was occupied by bread containing 1% HPMC. The results demonstrated that GF bread could be produced from a mixture of rice and millet flour and its technological quality was improved by using 1% HPMC and 3% CRJ. Therefore, it has the necessary potential for high-scale production and consumption among members of the society.

Novel Hydrolytic Degradable Crosslinked Interpenetrating Polymeric Networks (IPNs): An Efficient Hybrid System to Manage the Controlled Release and Degradation of Misoprostol.

The goal of this study was to make pH-sensitive HPMC/Neocel C19-based interpenetrating polymeric networks (IPNs) that could be used to treat different diseases. An assembled novel carrier system was demonstrated in this study to achieve multiple functions such as drug protection and self-regulated release. Misoprostol (MPT) was incorporated as a model drug in hydroxyl-propyl-methylcellulose (HPMC)- and Neocel C19-based IPNs for controlled release. HPMC- and Neocel C19-based IPNs were fabricated through an aqueous polymerization method by utilizing the polymers HPMC and Neocel C19, the initiator ammonium peroxodisulfate (APS), the crosslinker methylenebisacrylamide (MBA), and the monomer methacrylic acid (MAA). An IPN based on these materials was created using an aqueous polymerization technique. Samples of IPN were analyzed using scanning electron microscopy (SEM), atomic force microscopy (AFM), differential scanning calorimetry (DSC), thermal analysis (TGA), and powder X-ray diffraction (PXRD). The effects of the pH levels 1.2 and 7.4 on these polymeric networks were also studied in vitro and through swelling experiments. We also performed in vivo studies on rabbits using commercial tablets and hydrogels. The thermal stability measured using TGA and DSC for the revised formulation was higher than that of the individual components. Crystallinity was low and amorphousness was high in the polymeric networks, as revealed using powder X-ray diffraction (PXRD). The results from the SEM analysis demonstrated that the surface of the polymeric networks is uneven and porous. Better swelling and in vitro results were achieved at a high pH (7.4), which endorses the pH-responsive characteristics of IPN. Drug release was also increased in 7.4 pH (80% in hours). The pharmacokinetic properties of the drugs showed improvement in our work with hydrogel. The tablet MRT was 13.17 h, which was decreased in the hydrogels, and its AUC was increased from 314.41 ng h/mL to 400.50 ng h/mL in hydrogels. The blood compatibility of the IPN hydrogel was measured using different weights (100 mg, 200 mg, 400 mg, and 600 mg; 5.34%, 12.51%, 20.23%, and 29.37%, respectively). As a result, IPN composed of HPMC and Neocel C19 was successfully synthesized, and it is now possible to use it for the controlled release of MPT.

Effect of Additional Variations Hydroxyl Propyl Methyl Cellulose (HPMC) on Making of Patchouli Waxing Gel

Waxing gel is included in cosmetic epilation which can damage the skin barrier. To overcome this, it is necessary to add a composition that can moisturize, prevent irritation, and maximize its lifting power. In minimizing the possibility of irritation, it is necessary to add allantoin to waxing preparations as a calming agent that is safe for sensitive skin. The purpose of this study was to determine the effect of the of Hydroxyl Propyl Methyl Cellulose (HPMC) on the resulting waxing gel preparation including aroma, thickness, and maximum hair lift in certain areas of the body and to determine the best HPMC for removing unwanted hair. This type of research is experimental research with independent variables, namely HPMC variations of 0%, 1%, 2%, 3%, and 4%. The research procedure consists of preparation of tools, preparation of raw materials, and products produced. After that, several panelists made observations by giving questionnaires regarding aroma, viscosity and lifting power. The results showed that there was a comparative effect of the HPMC s used. Based on the observations of several panelists on the aroma, thickness, and lifting power of the waxing gel that has been made, it is known that at the HPMC 0% and 1% HPMC variables, it was found that many panelists stated that the waxing gel in these variables had a fragrant aroma, had a very rich texture. viscous and has very good lifting power compared to waxing gel variables , namely 2% HPMC, 3% HPMC, and 4%.

Extraction, Characterization, and Evaluation of Lepidium sativum Linn. Mucilage as a Mucoadhesive Polymer.

Being biocompatible, less toxic, cheap, easily available, and environmentally friendly, there is an increased trust in natural polymers in the drug delivery system. Mucilages, among the natural polymers, are the primary metabolites of plants that have been widely utilized in pharmaceutical manufacturing for different purposes, and mucoadhesive is one among them. The present study was designed to investigate the use of LSM as a mucoadhesive polymer using ibuprofen as a model drug. The mucilage was extracted following an aqueous extraction method and its percentage yield was found to be 13.2% w/w. Besides, three microsphere formulations of ibuprofen were prepared using synthetic polymer hydroxyl propyl methyl cellulose (HPMC) K100M and the LSM in polymer to drug ratios of 1 : 1, 1 : 5, and 3 : 5 by applying ionotropic gelation followed by solvent evaporation methods. The microspheres were evaluated for various micromeritic properties and all the formulations exhibited free-flowing properties. Optical microscopic pictures of almost all the microspheres except F3 and F6 (which had more or less spherical shapes) were found to have irregular and discrete shapes. Besides, the surfaces of all the formulations were rough in texture. The drug entrapment efficiency of the microspheres was found to be between 52.08% ± 0.80 and 87.97% ± 0.72. The in-vitrowash-off test evidenced that almost 50 percent (especially F3) of the microspheres were able to adhere up to 18 h and showed remarkable bioadhesion properties. The in-vitro drug release profile indicated that all the formulations were able to prolong their drug release up to 12 h with a non-fickian release mechanism, except for F4, which followed a fickian release. Therefore, based on the findings of this study, LSM can be used as a potential alternative mucoadhesive excipient for sustained release formulations.

Design and Characterisation of Rosuvastatin Calcium Nanosuspension Loaded Transdermal Patch

Objective: The present investigation highlights the formulation and evaluation of nanosuspension-loaded transdermal patches of poorly soluble antilipidemic drug (rosuvastatin) Methods: Dissolution characteristics of drug was improved by preparation of nanosuspension employing precipitation–ultrasonication technique using a different blend of water-soluble film forming polymers such as hydroxyl propyl methyl cellulose (HPMC K4M), Eudragit and were further characterized by fourier transformation infrared spectroscopy (FTIR), Malvern zetasizer and SEM. Propylene glycol and tween 80 were used as stabilizers. Based on the particle size of the formulation, the best one of NS4 was selected and fabricated into the transdermal patch by solvent casting method. The prepared formulations were evaluated for various parameters like drug excipient compatibility, appearance, morphology, thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, in-vitro drug permeation, and stability studies were performed for the optimized formula according to the ICH Q1A (R2) guideline under 4°C and 25°C RH for three months. Results: Amongst all formulation, P4 transdermal patches were considered the optimized formulation. It has the highest in-vitro drug permeation (86.01±0.05%), thickness (0.86±0.09), weight uniformity (475.0±8.60 mg), folding endurance (279.3±9.39), moisture uptake (7.06±1.75%), moisture content (6.81±2.34 %) and stable formula Conclusion: Therefore, transdermal patches were considered to be potentially suitable for the sustained release of drugs to improve patient compliance.

Buccal spray of standardized Berberis aristata extract causes tumour regression, chemoprotection and downregulation of inflammatory mediators in oral cancer hamster model

Ethnopharmacological relevanceBerberis aristata (BA) has been described in Ayurveda in formulations for treating conditions related to the buccal cavity, including tumours and inflammation. Oral cancer (OC) is a major global health problem with high rates of recurrence and metastasis. Natural product based therapies are being explored as safer therapeutic strategies for OC. Aim of the studyEvaluating the potential of standardized BA extract loaded buccal spray formulation in OC. Material and methodsBA stem bark extract was prepared using sonication and standardized with respect to Berberine. The standardized extract was characterized and formulated as a buccal spray (SBAE-BS) using hydroxyl propyl methyl cellulose K15M, polyethylglycol 400, Miglyol®812N and ethanol. The SBAE-BS was characterized and evaluated in vitro in KB cell line and in vivo in OC hamster model. ResultsThe SBAE-BS had pH, viscosity, mucoadhesive strength and BBR content corresponding to 6.8, 25.9 cP, 345 dyne/cm2 and 0.6 mg/mL respectively. In vitro cytotoxicity of SBAE-BS was comparable to 5 fluorouracil (5FU). In hamsters, SBAE-BS treatment lead to tumour regression (p = 0.0345), improved body weights (p < 0.0001), no organ toxicity, downregulation of inflammatory mediators and improved survival outcomes as compared to standard systemic 5FU. ConclusionThus, SBAE-BS showed cytotoxic and chemo-protective effects in the OC hamster model, evidencing its ethnopharmacological use and demonstrating translational potential to be developed as therapy for OC.

Evaluation of Khaya gum (Khaya senegalensis) as a polymer in the formulation of floating in situ gels of metoprolol succinate

Metoprolol succinate, a β-selectiveadrenergic blocker, has a short half-life, low bioavailability, and high dosingfrequency. In-situ gel drug delivery is a good approach to achieve sustained release for once-daily administration thatwill prolong drugretention time at the stomach and increase absorption. Thus,the aim of the study is to formulate floatingin-situ gel formulations of metoprolol succinate using Khaya gum (Khayasenegalensis, family Meliaceae) as a polymer. Khaya gum wascharacterized and used in formulating in situ gels of metoprololsuccinate in comparison with Hydroxyl Propyl Methyl Cellulose (HPMC K15M) andXanthan gum. The in-situ gel formulations were characterized forappearance, swelling, in- vitro buoyancy and in-vitro drugrelease. FTIR revealed major peaks characteristic of the gum. Khaya gum showedhigh swelling and good flow properties. In-situ gel formulations of metoprolol succinatecontaining Khaya were light brown with near neutral pH, higher swelling and a total floating time &amp;gt;24 h,comparable to those containing HPMC and Xanthan gums. Dissolution time t80was 60.50 to &amp;gt;240 min with ranking Khaya&amp;nbsp;&amp;lt;HPMC&amp;nbsp;&amp;lt;Xanthan. Khaya gum providesa cheaper, suitable polymer for formulating floating in-situ gels with prolonged buoyancy and drug release.

Fabrication of Polymeric Hydrogels Containing Esomeprazole for Oral Delivery: In Vitro and In Vivo Pharmacokinetic Characterization

Hydrogel is one of the most interesting and excellent candidates for oral drug delivery. The current study focuses on formulation development of hydrogels for controlled oral delivery of esomeprazole. The hydrogels were prepared by solution casting method by dissolving polymers in Polyvinyl alcohol (PVA) solution. Calcium alginate, Hydroxyl propyl methylcellulose (HPMC), acrylic acid and chondroitin sulfate were used in the preparation of hydrogels. Fourier transform infrared (FTIR) analysis showed no incompatibilities between drug and excipients used in the preparation of formulations. The hydrogels were characterized for size and surface morphology. Drug encapsulation efficiency was measured by Ultraviolet-visible (UV-VIS) spectroscopy. In vitro release studies were carried out using dissolution apparatus. The formulated hydrogels were then compared with the marketed product in vivo using rabbits. The result indicates that prepared hydrogels have a uniform size with a porous surface. The esomeprazole encapsulation efficiency of the prepared hydrogels was found to be 83.1 ± 2.16%. The esomeprazole-loaded hydrogel formulations showed optimum and Pharmacopeial acceptable range swelling behavior. The release of esomeprazole is controlled for 24 h (85.43 ± 0.32% in 24 h). The swelling and release of drug results make the prepared hydrogels a potential candidate for the controlled delivery of esomeprazole. The release of the drug from prepared hydrogel followed the super case transport-2 mechanism. The in vivo studies showed that prepared hydrogel formulations showed controlled and prolonged release of esomeprazole as compared to drug solution and marketed product. The formulations were kept for stability studies; there was no significant change observed in physical parameters, i.e., (appearance, color change and grittiness) at 40 °C ± 2/75% ± RH. There was a negligible difference in the drug content observed after the stability study suggested that all the formulations are stable under the given conditions for 60 days. The current study provides a valuable perspective on the controlled release profile of Hydroxyl propyl methylcellulose (HPMC) and calcium alginate-based esomeprazole hydrogels.

Duloxetine hydrochloride enteric-coated pellets in capsules with delayed release: formulation and evaluation

ABSTRACT The primary purpose of this study is to develop and evaluate an effective and reliable delayed-release dosage form of Duloxetine hydrochloride enteric-coated pellets in capsules. Duloxetine hydrochloride dissolves in an acidic environment, yet pellets maintain their enteric coating due to the Wurster expansion process for the Fluidized Bed Processor. Four distinct layers comprise enteric-coated pellets: a pharmaceutical layer, a barrier layer, an enteric layer, and a coating on the inert core pellets. A suspension layering approach protects the acidic environment from the drug by coating it with an enteric layer composed of hydroxyl propyl methyl cellulose phthalate HP55. We also determined the bulk and tapped densities, Hausner’s ratio, compressibility index, and moisture content of all formulations. The produced pellets are being evaluated for in-vitro release tests using UV-Visible spectroscopy. The zero-order model, the first-order model, and Higuchi’s square root equation, Hixson-Crowell, Korsemeyer peppas, and the Weibull model were used to evaluate the released kinetics models. Investigations using FT-IR (infrared spectroscopy) are still being undertaken to determine the drug’s compatibility with various excipients. Formulation ‘F7’ exhibited highest similarity factor of 56.1. Stability tests conducted over a three-month period under accelerated settings established that the optimized formulation is stable.

Formulation and evaluation of bi-layered tablet of divalproex sodium

Objective: To Formulate and Evaluate bi-layered tablet of Divalproex Sodium. Method: Divalproex sodium is broad-spectrum anticonvulsant. It increases the availability of gamma- amino butyric acid (GABA), an inhibitory neurotransmitter, The bilayer tablet of Divalproex sodium were prepared by using sodium starch glycolate, croscarmellose sodium, lactose, microcrystalline cellulose, polyvinyl pyrrolidone, magnesium stearate, talc, hydroxyl propyl methyl cellulose, as Excipents using wet granulation by using different Superdisintegrants. Result: In the present work, formulation and evaluation of bi-layered tablet of Divalproex sodium was carried out. In the project, different formulations of immediate release and sustained release layer have been prepared separately. From above formulations best formulation of each immediate and sustained release layers were selected according to the dissolution profile and bi- layered tablet were prepared. Conclusion: In the present work bi-layered tablet of Divalproex sodium were prepared by wet granulation method, using super disintegrants such as sodium starch glycolate and croscarmellose for immediate release layer and polymer like HPMC K4M and HPMC K100M for sustained release layer. Best formulations of each layer were selected for bi-layered tablet and bi-layered tablet were prepared. Bi-layered tablet of Divalproex sodium were subjected to hardness, weight variation, friability, drug content uniformity, in vitro drug release and drug polymer interaction.

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design.

Itraconazole (ITZ) is a triazole antifungal agent characterized by broad-spectrum activity against fungal infections. The main drawback of ITZ, when applied topically, is the low skin permeability due to the stratum corneum, the outermost layer of the skin, which represents the main barrier for drug penetration. Therefore, this study aimed to prepare itraconazole as transferosomes (ITZ-TFS) to overcome the barrier function of the skin. ITZ-TFSs were prepared by thin lipid film hydration technique using different surfactants, sodium lauryl sulfate (SLS) and sodium deoxycholate (SDC). The prepared ITZ-TFS were evaluated for entrapment efficiency (EE) %, particle size, polydispersity index (PDI), zeta potential, and in vitro drug release to obtain an optimized formula. The surface morphology of the optimized formula of ITZ-TFS was determined by transmission electron microscope (TEM). The optimized formulation was prepared in the form of gel using hydroxyl propyl methyl cellulose (HPMC) gel base. The prepared ITZ-TFS gel was evaluated for homogeneity, drug content, spreadability, pH, and in vitro antifungal activity in comparison with the free ITZ gel. The prepared ITZ-TFS formulations exhibited high EE% ranging from 89.02 ± 1.65% to 98.17 ± 1.28% with particle size ranging from 132.6 ± 2.15 nm to 384.1 ± 3.46. The PDI for all ITZ-TFSs was less than 0.5 and had a negative zeta potential. The TEM image for the optimized formulation (ITZ-TFS4) showed spherical vesicles with a smooth surface. The prepared gels had good spreadability, pH, and acceptable drug content. ITZ-TFS gel showed higher antifungal activity than free ITZ gel as determined by zone of inhibition. ITZ was successfully prepared in form of TFSs with higher antifungal activity than the free drug.

Comparison of pachymetry values during crosslinking with different riboflavin solutions

Objectives: To compare the effect of two different riboflavin solutions we use in the accelerated crosslinking (CXL) process on the pachymetry value. Materials and Methods: Patients who had accelerated CXL treatment with dextran-free riboflavin solution due to progressive keratoconus were retrospectively screened. Thirty-seven eyes of 27 patients (group 1) treated with Hydroxyl Propyl MethylCellulose (HPMC) and 0.1% riboflavin containing solution and 29 eyes of 23 patients (group 2) treated with D-alpha-tocopheryl polyethylene-glycol 1000 succinate (VE-TPGS) and 0.1% riboflavin containing solution were compared in terms of pachymetry changes during treatment. Results: In groups 1 and 2, the mean age was 23.92 ± 5.66 and 23.30 ± 4.89, respectively. Mean age, gender, initial keratometry values, mean central corneal thickness (CCT) before and after epithelial debridement did not differ significantly between the two groups. The CCT measured after riboflavin instillation was 453.22 ± 37.48 μ in the group 1 and 479.34 ± 38.54 μ in the group 2. After instillation of riboflavin, according to the initial CCT, there was an average thinning of 21.57 ± 16 μ in the group 1 and 18.72 ± 22.13 μ thickening in the group 2. According to the CCT measured after epithelial debridement, a thickening of 20.70 ± 21.77 μ in the group 1 and 62.76 ± 21.65 μ in the group 2 was observed. The rate of change of CCT after riboflavin instillation of significant differences existed between both groups. (p&lt;0.001). Conclusion: VE-TPGS, which is utilized to increase the cornea's permeability to riboflavin tissue during crosslinking treatment, significantly increases the corneal thickness compared to HPMC and provides a safer tissue thickness for ultraviolet A.

Design and characterization of fast dissolving buccal film of imipramine HCL

In depressed individuals, Imipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Imipramine hydrochloride having variable bioavailability i.e. ranging from 29-77% due to first pass metabolism, peak plasma concentration is usually attained 2-6 hours. Absorption is unaffected by food. It is freely soluble in water. The objective of this research work is to improve the bioavailability of the drug and fast the onset of action to decrease the depressant activity. The Buccal bioavailability of Imipramine HCL is only 29-77% for this reason drug can be administered into Buccal mucosa using mucoadhesive film. It can be made fast drug release and directly enter into blood circulation through Buccal mucosa and increase the drug bioavailability. Fast dissolving Buccal films were prepared by solvent casting method using various polymers like hydroxyl propyl methyl cellulose E15, PVP, PVA and sodium saccharin, plasticizer and vanillin as flavouring agent. Dissolution profile as studied in USP dissolution apparatus type 1 using pH 6.8 simulated saliva. The influence of variable like polymer type and concentration on Imipramine HCL release profile was studied. The formulation was optimized on the basis of various evaluation parameters like drug content and in vitro drug release. Formulation F3 successfully fast the release of drug within 8 minutes. The IR Spectra revealed the absence of interaction between drug and selected polymer, results of stability studies were as per ICH guide lines and results indicated that the selected formulation was stable.

Topical Formulation of Nano Spray-Dried Levocetirizine Dihydrochloride against Allergic Edema.

Levocetirizine dihydrochloride active ingredient was microencapsulated using nano spray-drying technology for preparing microparticles containing topical gel against edema. Hydroxyl propyl methyl cellulose (HPMC) was used as a carrier polymer during spray drying. The active ingredient content of the nano spray-dried products was 52.81% (w/w) and 51.33% (w/w) for ex vivo and in vivo experiments, respectively, and the average particle size was 2.6 µm. X-ray diffraction analysis indicated an amorphous state of the active ingredient embedded in the amorphous matrix of the polymer. Dermal oil gels composed of Miglyol 812 gelated by Dermofeel viscolid included 5% (w/w) (for ex vivo) and 10% (w/w) (for in vivo) active ingredient without or with 0.05% (w/w) menthol penetration enhancer. Qualitative ex vivo penetration studies using a confocal Raman microscopic correlation mapping were executed on human abdominal skin. The results showed that the active ingredient was enriched in the epidermis and upper dermis layer of the skin using oleogel loaded with the nano spray-dried drug-HPMC composite. Menthol addition to the oleogel resulted in the concentration of levocetirizine in the dermis. In vivo tests were performed on a mouse model of croton oil-induced ear edema. Negative control and Fenistil-treated groups were compared using the prepared oil gels with and without menthol. Without penetration enhancer, 20 µL of our oil gel loaded with nano spray-dried levocetirizine dihydrochloride composite showed similar effectiveness to the same volume of Fenistil gel, while 5 µL menthol containing sample was sufficient to eliminate the skin irritation similarly to 20 µL Fenistil.