FLUCONAZOLE NANOGEL: FABRICATION AND IN VITRO EVALUATION FOR TOPICAL APPLICATION

Objective: The aim of this study is to develop and in vitro evaluation of prepared fluconazole nanogel for seborrheic dermatitis Methods: Fluconazole nanogel was formulated to act against seborrheic dermatitis. The fluconazole nanoparticles were prepared by a simplified evaporation method and evaluated for particle size, entrapment efficiency, and percent in vitro drug release. The nanogel was also characterized based on parameters like particle size, percent entrapment efficiency, shape surface morphology, rheological properties, in vitro release R² = 0.9046, and release kinetics. Results: The nanoparticle with a combination of Eudragit RS and Tween 80 showed the best result with particle size in the range of 119.0 nm to 149.5 nm, with a cumulative percent drug release of 95 % up to 18 h. The formulated nanogel with optimum concentration of HPMC authenticate with particle size 149.50±0.5 with maximum drug release (92.13±0.32) %. Conclusion: Different percentages of polymers (ethyl-cellulose, eudragit, and tween 80) are used as variable components in the formulation of nanogel. The optimized batch showed good physical properties (flow index, spreadability, and viscosity) along with rapid drug release. Therefore, it can be concluded that nanogel containing fluconazole has potential application in topical delivery

FORMULATION AND OPTIMIZATION OF THERMOSENSITIVE IN-SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE FOR OCULAR DRUG DELIVERY

Objective: The present study has focused on development and optimization of thermosensitive in-situ ocular drug delivery system for the treatment of conjunctivitis.Methods: Thermosensitive in-situ hydrogel formulation of moxifloxacin hydrochloride was developed by dispensing variable concentration of pluronic F-127, gellan-gum, and carbopol in distilled water. Viscosity, gelation temperature and mean release time (MRT) were measured by using ‘Brookfield' viscometer LV-III (spindle no. 40), rheological techniques and dissolution apparatus respectively. Optimization for ideal formulation was carried by ‘Box–Behnken' design on the basis of prime factors of the formulation including viscosity, gelation temperature, and MRT. Moreover, the optimized formulation was evaluated for accelerated stability study by in vitro drug release, anti-microbial potential by ‘Kirby-Bauer disk diffusion' method and ocular irritancy assay were done by in vivo analysis.Results: Optimised thermosensitive in-situ gel, when administered into cul-de-sac region of the eye, it was immediately transformed from sol to gel by multi-dimensional mechanism due to plurionic, gellan-gum, carbopol. The optimized formulation minimizes the chances of formulation failure as well as the concentration on individual polymer which dependence on a single mechanism of gelation. The final optimised formulation consists of plurionic (11.50% w/v), gellan-gum (0.32% w/v), carbopol (0.3% w/v), shows optimum therapeutic effect. Moreover, the accelerated stability study, anti-microbial potential, and ocular irritancy confirmed the biocompatibility of optimized in-situ drug-containing gel with high potency and stability.Conclusion: Thus, optimized in-situ drug-containing gel with multifactorial approaches showed promising ocular formulation having minimum side effect and high therapeutic efficacy.Â

PREPARATION AND EVALUATION OF COPPER NANOPARTICLES LOADED HYDROGEL FOR BURNS

Objective: The present study focuses on the development and optimization of copper nanoparticles (CNPs) loaded hydrogel for the treatment of dermal burn injuries. Methods: CNPs gel was prepared by dispersing the variable concentration of polyvinylpyrrolidone (PVP K30) and hydroxypropyl methylcellulose (HPMC) in distilled water, PEG 400, and copper nanoparticles. factor screening study was performed for identification of influential factors, followed by optimization study using three-factor Box-Behnken design. Results: Optimized nanogel formulation, when compared to normal control (NC), shows a significant reduction of pro-inflammatory cytokines (IL-6 = 39.74 % and TNF-α =49.37%) and increased level of anti-inflammatory cytokines (IL-10 = 30.90%), indicating reduced inflammation. Further, the wound closure rate of CNPs gel shows significant (12.27 %) wound closure as compared to the NC group and complete wound closure (100 %) on the 14th day, indicating accelerated wound healing. Conclusion: the present investigation endorses accelerated scar-free, accelerated wound healing potential of copper nanoparticles gel with anti-inflammatory potential

Ácido glicirrícico: extracción, cribado y evaluación de la propiedad anti-inflamatoria

The authors wish to thank Founder President Dr. Ashok K. Chauhan, Amity University for his kind support during the researchObjective: Glycyrrhizic acid is a widely used medicinal component as an anti-inflammatory agent, anti ulcer agent, anti-allergy agent and anti-psoriatic agent. The present investigation deals with the extraction of glycyrrhizic acid from licorice roots and evaluating its in-vitro anti inflammatory activity. Methods: Glycyrrhizic acid was extracted using the procedure of maceration. The extract was evaluated for its physicochemical property, biochemical tests and phytochemical properties. The Ii vitro anti- inflammatory activity was evaluated by albumin denaturation technique Results: The results showed that the ash value and the extractive values for the extract were found to be in the limit as given by Ayurvedic Pharmacopoeia of India. Presence of flavonoids, saponins and triterpinoids were identified in the extract from phytochemical parameters. Thin layer chromatographic technique showed a retention value of 0.5 cm. The percentage inhibition showed that the extract is having some potential of healing inflammation. Conclusion: Glycyrrhizic acid was successfully extracted from licorice roots. The evaluation parameters showed the presence of less impurity in the extract, with the potential of having anti-inflammatory property.Objetivo: El ácido glicirrícico es un componente medicinal ampliamente utilizado como agente antiinflamatorio, agente antiulceroso, agente antialérgico y agente anti-psoriásico. La presente investigación trata de la extracción de ácido glicirrícico a partir de raíces de regaliz y la evaluación de su actividad antiinflamatoria in vitro. Métodos: el ácido glicirrícico fue extraído usando el procedimiento de la maceración. El extracto fue evaluado por su propiedad fisicoquímica, pruebas bioquímicas y propiedades fitoquímicas. La actividad antiinflamatoria in vitro fue evaluada por la técnica de desnaturalización de albúmina Resultados: los resultados demostraron que el valor de la ceniza y los valores extractivos para el extracto se encontraron en el valor límite según lo dado por la farmacopea de Ayurveda de la India. La presencia de flavonoides, de saponinas y de triterpenoides fue identificada en el extracto mediante parámetros fitoquímico. La técnica cromatográfica en capa delgada demostró un valor de retención de 0,5 centímetros. La inhibición porcentual mostró que el extracto tiene algún potencial de curación de la inflamación. Conclusión: el ácido glicirrícico fue extraído con éxito de las raíces de regaliz. Los parámetros de evaluación mostraron la presencia de menos impureza en el extracto, con el potencial de tener propiedades antiinflamatorias

FORMULATION, OPTIMIZATION, AND EVALUATION OF IN-SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE FOR OPHTHALMIC DRUG DELIVERY

Objective: The present study emphasizes the synthesis, optimization, and evaluation of ocular in-situ gel for ophthalmic drug delivery against conjunctivitis. Methods: Pre-formulation studies on the drug and polymers were carried out, which included the study of various physicochemical properties of the drug and drug-polymer compatibility studies. The 12 different formulations were further pre-optimised by Taguchi method for determining the number of influential factors. Furthermore, the formulation optimization was done by using ‘Box–Behnken’ design (BBD) (Design expert 10 software) for assessing the effect of formulation variables on product characteristics viz. viscosity, gelation temperature (GT), and mean release time (MRT). About 13 suggested runs of the experiment were carried out and formulations were optimised. Finally, three batches of the optimised formulation were prepared and evaluated for in vitro drug release, isotonicity of formulation, anti-microbial potential, ocular irritancy, and accelerated stability testing. Results: Pre-formulation study confirmed the purity, solubility, and compatibility of drug measured by λmax, partition coefficient, stability study, and Fourier-transform infrared spectroscopy (FTIR) analysis. Taguchi screening method suggested about 12 different formulations and 3 most prominent influential factors including viscosity, GT, and drug release. 13 different formulations designed based on ‘BBD’ method were further optimised by considering the most influential factors suggested by Taguchi screening. The in vitro evaluation of the optimised formulation gave satisfactory results in terms of drug release, and anti-microbial activity. It was found to be isotonic with no ocular irritancy. Further, the preparation immediately transformed from sol to gel upon administration into cul-de-sac region of the eye due to multi-dimensional approaches utilised for in-situ gel formation namely temperature change Pluronic, ion sensitivity due to Gellan-gum, pH sensitivity because of Carbopol. Conclusion: The optimised in-situ gelling ocular drug formulation showed promising potency for ophthalmic drug delivery with no irritancy due to the multifactorial mechanism

THERAPEUTIC EVALUATION OF CHEMICALLY SYNTHESIZED COPPER NANOPARTICLES TO PROMOTE FULL-THICKNESS EXCISIONAL WOUND HEALING

Objective: The purpose of this research was, synthesis of copper nanoparticles using environment friendly cementation method and evaluate their wound healing property on full-thickness excisional wound. Methods: Present study reports the synthesis of CNPs by single-step cementation method. Evaluation of CNPs was endorsed by morphological and chemical properties. Furthermore, CNPs was evaluated for its antibacterial potential and invitro hemocompatibility. Additionally, pharmacological evaluation of CNPs was assessed against excisional wound. Results: Characterization of final product indicate, particle size of CNPs were ranging from 100-150 nm. CNPs showed significant antibacterial activity (A= 2.1±0.1 mm, B =2.1±0.1 mm, C = 1.9±0.2 mm, at 10µg/ml), along with superior hemocompatibility (RBC cell survival 97±1 %). Further CNPs formulation shows increased level of anti-inflammatory cytokinin’s (IL-10, 42.7%) as compared to standard (STD), vehicle control, and normal control groups, attributed to accelerated wound healing (p<0.05 vs STD). Conclusion: The consequences the present investigation endorse the accelerated wound healing potential of CNPs with its anti-inflammatory potential

Fabrication and in vitro characterization of polymeric nanoparticles for Parkinson's therapy: a novel approach

O objetivo da pesquisa foi formular e avaliar nanopartículas de quitosana contendo cloridrato de selegilina para terapia do Parkinson, a fim de melhorar o seu efeito terapêutico e reduzir a frequência de dosagem. Método de Taguchi, de planejamento experimental, (L9 matriz ortogonal) foi usado para obter a formulação otimizada. As nanopartículas de quitosana contendo cloridrato de selegilina (PCHs) foram preparadas por gelificação iônica de quitosana com ânions tripolifosfato (TPP) e Tween 80 como tensoativo. As PCHs apresentaram tamanho médio de (303.39 ± 2,01) nm, potencial zeta de +32.50 mV e eficiência de encapsulação de 86.200±1,38%. A liberação do fármaco in vitro foi avaliada em solução salina de tampão fosfato (pH 5,5), usando a mucosa nasal de cabra e o resultado encontrado foi de 82.529% ± 1.308, acima de 28 h. Estudos de cinética de liberação mostraram que a liberação do fármaco das nanopartículas foi por difusão anômala (não fickiana), indicando que é controlada por mais de um processo, ou seja, a superposição dos fenômenos de difusão controlada e intumescimento. As PCHs mostraram resultados de boa estabilidade, encontrada durante os estudos de estabilidade em temperaturas diferentes, como mencionado em diretrizes do ICH. Os resultados revelaram que o sistema de nanopartículas de quitosana contendo cloridrato de selegilina é o mais adequado sistema de liberação de fármacos de ação terapêutica promissora.The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action

Sistema de administración tópica basada en microesponjas de miconazol para la dermatitis del pañal

Objetivo: La presente investigación tuvo como objetivo desarrollar y optimizar las microesponjas de nitrato de miconazol para el tratamiento de la dermatitis del pañal para un efecto terapéutico mejorado. Material y métodos: Las microesponjas fueron desarrollados por emulsión técnica de difusión del disolvente usando un diseño factorial 23. Las microesponjas fabricadas han sido optimizadas con el fin de analizar los efectos de las variables independientes sobre la eficacia de encapsulación, tamaño de partícula, la topografía de la superficie y en la liberación de fármaco in vitro. A continuación, la formulación optimizada se incorporo en un gel y se evaluó. Resultados: Se encontró que el tamaño de partículas de todas las formulaciones fue uniforme y la microscopía electrónica de barrido (SEM) indicó forma esférica y de naturaleza porosa de las microesponjas. En la liberación del fármaco, estudios in vitro de todas las formulaciones, revelaron la velocidad de liberación dentro de un intervalo de 67±0,09% a 80,6±0,68% al cabo de 12 horas. Con esta base, La formulación F8 se seleccionó y se incorporó en el gel (CF8) en el que se evaluó el pH, viscosidad, capacidad de extensión, estudios de difusión in vitro del fármaco, estudios in vitro anti hongos y estudios de estabilidad. Conclusión: El gel a base de microesponja formulado de nitrato de miconazol sería un sustituto adecuado al tratamiento tradicional para la curación fiable y económica de la dermatitis del pañal.Aim: The current investigation was aimed to develop and optimize the microsponges of miconazole nitrate for treatment of diaper dermatitis for enhanced therapeutic effect. Material and Methods: Microsponges were developed by emulsion solvent diffusion technique using 23 factorial design. Fabricated microsponges were optimized in order to analyze the effects of independent variables on the encapsulation efficiency, particle size, surface topography and in vitro drug release. The optimized formulation was then incorporated into the gel and evaluated. Results: Particle size of all formulations was found to be uniform and scanning electron microscopy (SEM) indicates spherical shape and porous nature of microsponges. In vitro drug release studies of all formulations revealed the release rate within the range of 67%±0.09 to 80.6%± 0.68 at the end of 12 hours. On its basis, formulation F8 was selected and incorporated into the gel (CF8) which was evaluated for pH, viscosity, spreadability, in vitro drug diffusion studies, in vitro anti fungal studies and stability studies. Conclusion: The formulated microsponge-based gel of miconazole nitrate would be a capable substitute to traditional treatment for reliable and economical cure of diaper dermatitis

DEVELOPMENT AND CHARACTERIZATION OF SUSTAINED RELEASE METHOTREXATE LOADED CUBOSOMES FOR TOPICAL DELIVERY IN RHEUMATOID ARTHRITIS

Objective: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are essential part of the administration of Rheumatoid Arthritis (RA). Methotrexate (MTX) is effective for tumor necrosis factor alpha (TNF-a) biologic agents, indicated only in minority of patients suffering from severe RA. MTX remains the "anchor drug" in the treatment of RA. For delivery improvement, novel pharmaceutical drug delivery system i.e. MTX-Cubosomes were developed. Methods: Poloxamer 407 and Glycerol monooleate (Monoelin, MO) used and the formulation were characterized as a sustained release drug delivery system for Methotrexate. Different ratios of Monolein, Poloxamer 407 and water were used to develop the different cubosomes using homogenization and emulsification method. Characterization of formulations for morphology was performed and also particle size distribution by Transmission Electron Microscopy (TEM). Results: Formulation showed the internal cubic structures of the vesicles. The particle size of the formulations was found to be ranging from 53.21 to 185.32 nm, zeta potential of the formulations varied from-18.20-36.10 mV. The cubosomal formulation exhibited good entrapment efficiency along with high drug loading. Compatibility with the excipients was also established. An in vitro release study was done using Franz Diffusion cell indicated sustained release of the formulation at a rate of 1.25 %/h. Cubosomes proved to be reliable system for sustained transdermal drug delivery system. Conclusion: Methotrexate cubosomes is a novel medication delivery framework and in this examination it has been developed and characterized. The formulations were found to be promising in terms of its characterization parameters like particle size, zeta potential, entrapment efficiency, loading capacity, release kinetics, and stability, suitable for topical delivery

Design, development and in vitro characterization of Pioglitazone loaded mucoadhesive buccal devices

Aim: The mucoadhesive buccal patches were developed and evaluated for systemic administration of Pioglitazone in the oral cavity. Pioglitazone belongs to a novel class of oral antidiabetic drugs known as Thiazolidinediones. Materials and Methods: The mucoadhesive buccal patches of Pioglitazone was formulated using Eudragit RS100 and HPMC K4M (mucoadhesive polymer) and were prepared by solvent casting method. Different patch formulations were evaluated for its physical parameters like thickness uniformity, swelling index, surface pH, uniformity of weight, folding endurance, mucoadhesive strength and in vitro parameters like drug content uniformity and drug release studies, and ex vivo parameters like mucoadhesion time. Results: Data for the parameters was found to be: thickness uniformity (0.27±0.45mm); uniformity of weight (40.81±0.66 mg), surface pH (6.5), folding endurance (>300), drug content uniformity (98.58±2.05%), swelling index (131±0.79%), mucoadhesive strength (38.20±1.75), in vitro drug release studies (95.18±1.98%) and ex vivo mucoadhesion, time of optimized formulation (4±1.26 h). The data was also fitted to different kinetic models to illustrate its anomalous (non-fickian) diffusion. Conclusions: The result revealed that Pioglitazone loaded buccal patches was most suitable mode of drug delivery for promising therapeutic action. Buccal patches of Pioglitazone can prove to be potential pharmaceutical dosage form for sustaining the drug release and reducing the dose frequency.Objetivo: Los parches de mucoadherente bucal fueron desarrollados y evaluados por la administración sistémica de la pioglitazona en la cavidad oral. Pioglitazona pertenece a una clase nueva de medicamentos antidiabéticos orales conocida como tiazolidindionas. Material y Método: los parches mucoadherente bucal de pioglitazona fue formulado con Eudragit RS100 y HPMC K4M (polímero mucoadherentes) y fueron elaboradas por el método de fundición solvente. Se evaluaron diferentes formulaciones de parches mediante parámetros físicos como uniformidad de espesor, índice de hinchazón, pH de la superficie, uniformidad de peso, resistencia al plegado, fuerza mucoadherentes y parámetros in vitro como uniformidad de contenido del fármaco y estudios de liberación y estudios ex vivo del tiempo de mucoadhesión del fármaco. Resultados: Los resultados obtenidos para los parámetros estudiados fueron: uniformidad de espesor, 0.27±0.45 mm; uniformidad de peso, 40.81±0.66 mg; pH superficial, 6.5; resistencia al plegado, > 300. Los ensayos in vitro dieron los siguientes resultados: uniformidad de contenido del fármaco, 98.58±2.05%; índice de hinchazón, 131±0.79%; fuerza mucoadherente, 38.20±1.75; y tiempo de liberación del farmaco (95.18±1.98%) y el ensayo ex vivo del tiempo de mucoadhesión del fármaco fue de 4±1.26 h. Los datos también se ajustaron a distintos modelos cinéticos para ilustrar su difusión anómala (no Fickian). Conclusiones: El resultado reveló que los parches bucales de pioglitazona fue el modo más adecuado de fármacos de acción terapéutica prometedora. Los Parches bucales de pioglitazona pueden resultar una potencial forma de dosificación farmacéutica para sostener la liberación del fármaco y reducir la frecuencia de la dosis.The authors are thankful to Panacia Biotec, Baddi (H.P.) India for providing the Pioglitazone as a gift sample. We are also thankful to the Board of Trustees, Bharat Institute of Technology, Meerut, India for providing necessary facilities to carry out this research work