Formulation of Mesalamine-Loaded Rectal Mucoadhesive Pellets for the Treatment of Inflammatory Bowel Disease Using 32full Factorial Design

Abstract

Objective: The objective of the present work was to optimize a rectal suppository containing mucoadhesive pellets of Mesalamine to achieve local yet sustained release of Mesalamine for once-a-day administration for the therapy of Inflammatory Bowel Disease. Methods: Thus, the present work involves forming mucoadhesive pellets of mesalamine by extrusion spheronization, which were then loaded into a suppository to be administered rectally. The pellets were evaluated for mucoadhesion strength, swelling potential, morphology, particle size, drug release, drug loading and retention time. Results: The optimized batch of pellets using Eudragit RLPO as the release retardant, carrageenan as a mucoadhesive polymer and other excipients had a mucoadhesion strength of 0.143 N, a swelling index of 50.50 %, and 44 % and 75 % drug was released from them at the end of 6 and 15 h respectively. The pellets-loaded cocoa butter suppositories had a melting range of 35–37 °C, disintegrated within 8–9 min and had a hardness of 4–5 kg/cm3. A comparison of the in vitro drug release profile from the mucoadhesive pellets and the mucoadhesive pellets-loaded suppositories showed a closeness in the % cumulative drug release indicating that cocoa butter did not interfere in the release of the drug from the pellets. Conclusion: Mucoadhesive Pellets were successfully developed by extrusion spheronizer technique and incorporated into suppositories. In vitro study revealed a release profile that warranted a once-a-day regimen leading to a reduction in the requirement of the drug and hence the side effects.

Quality by Design-Driven Formulation Development and Optimization of Enalapril Maleate Loaded Mucoadhesive Microspheres: In Vitro and in Vivo Characterization

“…Administration of enalapril maleate in sustain release dosage mucoadhesive microspheres as once daily dose would be further enviable since this formulation is proposed to be given to the patients for the management of essential and reno-vascular hypertension and cardiac congestion. The objective of the study is to design a sustained release mucoadhesive microspheres using sodium alginate along with HPMC K4M mucoadhesive polymer to liberate the drug slowly over an extended period for the improvement of therapeutic efficacy and patient compliance [8,9].…”