Development of Emulgel Delivery of Mupirocin for Treatment of Skin Infection

2020 ◽  
Vol 15 (2) ◽  
pp. 137-156
Author(s):  
Swati C. Jagdale ◽  
Payal V. Kothekar
Keyword(s):  
Staphylococcus Aureus ◽  
Controlled Release ◽  
Skin Infection ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Topical Delivery ◽  
Antibacterial Drug ◽  
Batch Release ◽  
Anti Inflammatory ◽  
Excipient Compatibility

Aim:: To design controlled release topical delivery of mupirocin for the treatment of skin infection. Background:: Mupirocin is an antibacterial drug. Mupirocin works to kill the bacteria, which include strains of Staphylococcus aureus and Streptococcus pyogenes. It is also used for the treatment of inflammation of a hair follicle. The half-life of mupirocin is only 20-40 min. It has very slight solubility in water. Patent literature had shown work on ointment, antibiotic composition, nasal and topical composition. Emulgel is a duel control release system for the topical delivery of hydrophobic drugs. Objective:: The objective was to formulate emulgel with controlled delivery of mupirocin using Sepineo P 600. Methods:: Soya oil, tween 80 and polyethylene glycol 400 (Oil:Surfactant:Cosurfactant) were used for emulsion formulation. Emulgel was optimized by 32 factorial design. Sepineo P 600 and hydroxy propyl methyl cellulose K4M were used as independent variables. Drug excipient compatibility analysis was carried out by FTIR, UV and DSC spectra. Emulgel was evaluated for its physical characterization, in vitro release, ex vivo release, antimicrobial and anti-inflammatory study. Results:: DSC, UV and FTIR analysis confirmed drug excipient compatibility. FE SEM showed a size range between 228-255 nm. Zeta potential was found to be -25.1 mV, which showed good stability of the emulsion. Design expert software showed F2 as an optimized batch. Release studies indicated that the controlled release of drugs forms Sepineo P 600 gel due to its higher gelling capacity. Batch F2 showed comparable results with marketed formulation against Staphylococcus aureus. For batch F2, 40 μg/ml was the minimal inhibitory concentration. Conclusion:: Antimicrobial and anti-inflammatory study proved successful development of stably controlled release mupirocin emulgel.

scholarly journals Formulation and in vitro evaluation of metformin hydrochloride loaded microspheres prepared with polysaccharide extracted from natural sources

2013 ◽  
Vol 63 (2) ◽  
pp. 209-222 ◽  
Author(s):  
Hemanta Kumar Sharma ◽  
Sunita Lahkar ◽  
Lila Kanta Nath
Keyword(s):  
Controlled Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Rice Flour ◽  
Metformin Hydrochloride ◽  
Natural Sources ◽  
Natural Materials ◽  
Diffusion Technique ◽  
Excipient Compatibility

The present work envisages utilisation of biodegradable and biocompatible material from natural sources for the development of controlled release microspheres of metformin hydrochloride (MetH). Natural polysaccharides extracted from Dillenia indica L. (DI), Abelmoschus esculentus L. (AE) and Bora rice flour were used in fabricating controlled release microspheres. The microspheres were prepared by the emulsion solvent diffusion technique with different proportions of natural materials and were studied for entrapment efficiency, particle size, particle shape, surface morphology, drug excipient compatibility, mucoadhesivity and in vitro release properties. The prepared microspheres showed mucoadhesive properties and controlled release of metformin hydrochloride. The study has revealed that natural materials can be used for formulation of controlled release microspheres and will provide ample opportunities for further study

scholarly journals LORNOXICAM-LOADED NANOSPONGES FOR CONTROLLED ANTI-INFLAMMATORY EFFECT: IN VITRO/IN VIVO ASSESSMENT

2020 ◽  
pp. 217-223
Author(s):  
SEHAM M. SHAWKY ◽  
MAHA K. A. KHALIFA ◽  
HEBA A. EASSA
Keyword(s):  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Inflammatory Activity ◽  
Carboxymethyl Cellulose Sodium ◽  
Anti Inflammatory

Objective: To design a controlled topical delivery system of lornoxicam (LX) in order to enhance skin permeation and treatment efficacy. Nanosponges were selected as a novel carrier for this purpose. Methods: Nanosponges were formulated via the emulsion solvent evaporation method using ethyl cellulose (polymer) and polyvinyl alcohol (surfactant). Nanosponge dispersions were characterized for colloidal properties, entrapment efficiency and in vitro release study. The nanosponge formulation (LS1) was then incorporated into carboxymethyl cellulose sodium hydrogels and evaluated for pH, viscosity and in vitro drug release. Skin irritation was evaluated, and anti-inflammatory activity was assessed via rat hind paw edema method. Results: Nanosponges were in the nano-sized range and attained a uniform round shape with a spongy structure. LS1exhibited the highest LX release after 6 h, so it was incorporated as hydrogel. Formulated hydrogels showed acceptable physicochemical parameters (pH, drug content and rheological properties). Skin irritation testing proved LX-loaded nanosponge hydrogel formulation (G1) to be non-irritant. In vivo study revealed an enhanced anti-inflammatory activity of G1 for 6 h (p<0.001). Conclusion: The developed nanosponge hydrogel is an efficient nanocarrier for improved and controlled topical delivery of LX.

Development and Evaluation of Olmesartan Medoxomil Controlled Release Floating Microspheres using Natural Gums

2017 ◽  
Vol 10 (4) ◽  
pp. 3788-3794
Author(s):  
Ravi Kumar Kota ◽  
Suresh Gande
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Olmesartan Medoxomil ◽  
In Vitro Dissolution ◽  
Coupled Diffusion ◽  
Intact Surface

The present research was aimed to prepare Olmesartan medoxomil floating microspheres for controlled release using polymers such as sodium alginate, sodium bicarbonate, calcium chloride, Hydroxy propyl methyl cellulose (HPMC K4M, K15M), Olibanum gum and Xanthan gum by ionotropic gelation method. The prepared microspheres were evaluated for the percent drug content, entrapment efficiency, percentage buoyancy and in vitro dissolution studies. Among all the formulations F14 was selected as optimized formulation based on the micromeretic and physico-chemical parameters including drug release studies. Percentage buoyancy of optimized formulation was found to be 96.45%. In vitro release study of formulation F14 showed 98.11% drug release after 12 h in a controlled manner, which is desired for disease like Hypertension.  The reference standard shows the drug release of 94.12% within 12 h. Drug and excipient compatibility studies were carried out by FT-IR and no interactions were observed. The SEM of microspheres show a hollow spherical structure with a rough surface morphology. Some of microspheres showed dented surface structure but they showed good floating ability on medium indicated intact surface. The shell of microspheres also showed some porous structure which might be due to release of carbon dioxide. F14 followed zero order, Higuchi and Korsmeyer Peppas kinetics indicating diffusion controlled with non-fickian (anomalous) transport, projecting that its active ingredient are delivered by coupled diffusion and erosion. From these results, it can be concluded that the polymer proportion controlled the drug release from the olmesartan floating microspheres. 

scholarly journals Preparation, Characteristics, and Controlled Release Efficiency of the Novel PCL-PEG/EM Rod Micelles

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Huiling Song ◽  
Yu Yin ◽  
Jiahui Peng ◽  
Zixiu Du ◽  
Wei Bao
Keyword(s):  
Staphylococcus Aureus ◽  
Controlled Release ◽  
Encapsulation Efficiency ◽  
Orthogonal Design ◽  
Drug Loading ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Average Particle ◽  
Model Drug

In order to achieve sustained and controlled release of the hydrophobic cargoes, improve the bioavailability, and reduce the side effects of antibiotics, the model drug erythromycin (EM) was used to prepare polycaprolactone-polyethylene glycol (PCL-PEG)/EM micelles. PCL-PEG, a biocompatible and biodegradable amphiphilic polymer, was used as carrier material of micelles to optimize the formulation and preparation process by orthogonal design. The morphology, stability, drug loading, and encapsulation efficiency and the in vitro release behavior of the micelles were investigated. In addition, activity assays of anti-Staphylococcus aureus were performed. The results indicated that PCL-PEG/EM were rod-like micelles with an average particle size of 220 ± 2.6  nm and a zeta potential of +19 mV. The average drug loading and encapsulation efficiency were approximately 6.5% and 97.0%, respectively. The micelles were stable in the serum within three days. At the effective concentration of the drug, the formulation indicated no apparent toxicity to the cells. The micelles were able to rapidly enter Staphylococcus aureus (S. aureus) and to provide sustained release cargoes that effectively inhibited S. aureus proliferation. The present study provided a new platform for the rational and effective use of hydrophobic antibiotics to treat infections.

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

Microsponges: An Overview

2017 ◽  
Vol 4 (4) ◽  
Author(s):  
Hamid Hussain ◽  
Divya Juyal ◽  
Archana Dhyani
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Oral Delivery ◽  
Active Agent ◽  
Topical Delivery ◽  
Water Soluble ◽  
Wide Range ◽  
Porous Beads

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by difussion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.

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