Preparation, Optimization, and Evaluation of Pellets Containing Mesalamine With Natural Gums For Colon Drug Delivery System

Year 2022, Volume: 1 Issue: 47, 35 - 56, 01.03.2022

Rijawan Rajjak Pathan Aquil-ur-rahim Sıddıquı

https://doi.org/10.55262/fabadeczacilik.1078778

Cited By: 2

Abstract

The purpose of the present work was to formulate colon-targeted mesalamine pellets containing gums of Moringa oleifera Lam. (MOG) and Cyamopsis tetragonolobus Taub. (CTG). Formulation of single stimuli mediated release is also difficult to target colon due to variation in the physiological condition, so in present work, pH dependent and enzyme degradation mechanisms are being used to release of drug at the colonic site. Extrusion and spheronization techniques were used for the preparation of pellets. For formulation optimization, factorial design study 32 was used for the selection of the optimized batch. It was found that high ratio of solvent 80:20 and 10% and 7.5% concentration of MOG and CTG respectively produce optimized pellets showed good physical properties and release for F8M and F8C and after coating it showed in vitro release at the colonic condition and in vivo roentgenographic images for targeting. As to say as advantages, spheronization and extrusion method was proved to have economized, whereas natural gums used to control
release which added advantage as being as inert and biocompatible. This further formulation scope at industrial scales to reduce side effects of synthetic polymer and make it more biocompatible with the body.

Keywords

Mesalamine, pellets, Moringa oleifera gum, Cyamopsis tetragonolobus gum, in vivo colon targeting

Kolona Hedefli Doğal Sakız ve Mesalamin İçeren Pelletlerin Hazırlanması, Optimizasyonu ve Değerlendirilmesi

Abstract

Bu çalışmanın amacı Moringa oleifera Lam. (MOG) ve Cyamopsis tetragonolobus Taub. (CTG)’ den elde edilen sakızları içeren kolona hedefli mesalamin pelletlerinin hazırlanmasıdır. Tekli uyaran aracılı salımın kolona hedefli olarak gerçekleştirilmesinin fizyolojik koşullardan dolayı zor olması nedeniyle salımın kolonda sağlanması için pH ve enzime duyarlı salım mekanizmaları kullanılmıştır. Pelletlerin hazırlanmasında ekstrüzyon ve sferonizasyon teknikleri kullanılmıştır. Formülasyonun optimizasyonunda, optimize serinin seçimi için faktöriyel tasarım çalışması 32 kullanılmıştır. Yüksek çözücü oranı (80:20) ve MOG ve CTG’nin sırasıyla %10 ve %7.5 konsantrasyonlarda kullanımının optimize pelletlerin elde edilmesini
sağladığı saptanmıştır. Elde edilen optimize pelletler hedeflendirme için iyi fiziksel özellik göstermiş ve F8M ve F8C formülasyonları ve bunların kaplanmış formülasyonları kolon ortamında iyi in vitro salım özelliği göstermiş ve in vivo röntgenografik görüntü vermiştir. Avantaj olarak söylemek gerekirse, sferonizasyon ve ekstrüzyon ekonomik açıdan avantaj sağlarken kontrollü salım sağlamak amacıyla kullanılan doğal kaynaklı sakızlar inert ve biyouyumlu yapıları ile avantaj sağlamıştır. Bu formülasyon, endüstriyel ölçeklerde sentetik polimerin yan etkilerini azaltıp vücutla daha biyouyumlu hale getirebilir.

Keywords

Mesalamin, pelletler, Moringa oleifera zamkı, Cyamopsis tetragonolobus zamkı, in vivo kolon hedefleme.

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