Formulation development of gastroretentive tablets of lamivudine using the floating-bioadhesive potential of optimized polymer blends

Abstract

Besides unravelling the polymer synergism, the study helped in developing an optimal once-a-day gastroretentive drug delivery system with improved bioavailability potential exhibiting excellent swelling, floating and bioadhesive characteristics.

QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

“…The latter curve, however, exhibited significantly improved fitting with quadratic model demonstrating the prevalence of nonlinearity (r=0.894; p<0.01). The prevalence of such nonlinear pattern is in accordance with the literature studies reported for fast release formulations (1,40). Besides exploring the magnitudinal relationship between the in vitro and in vivo data, the establishment of IVIVC also ratifies the apt selection of in vitro dissolution conditions like, dissolution apparatus, media composition, and time-points for predicting the in vivo pharmacokinetic performance (8,41).…”

“…The extent of drug absorption, as revealed by the AUC 24h values, was also found to be significantly higher from the optimized formulation than from the marketed formulation (i.e., 1.78-fold; p<0.001). Such enhancement in the bioavailable fraction is in consonance with several of previous reports on GR formulations (1,8,38,39). Overall, the studies construe appreciable extension in drug absorption profile when formulated as floating-bioadhesive tablets, ostensibly owing to the increase in gastric residence time by virtue of its floatation and bioadhesion characteristics.…”

“…These limitations can largely be overcome by developing the floating systems coupled with mucoadhesion Electronic supplementary material The online version of this article (doi:10.1208/s12249-015-0431-9) contains supplementary material, which is available to authorized users. characteristics to adhere the dosage form to the mucous lining of stomach wall (1,8). The floating-bioadhesive systems therefore greatly improve the residence time of the drug resulting in effective extension in the absorption and oral bioavailability.…”

“…In this regard, oral controlled release (CR) formulations are primarily employed for reducing the frequency of administration by regulating the drug release rate for prolonged periods of time, thus improving the patient compliance (1,2). However, development of CR products is precluded by their inability to retain the formulation within the desired region of gastrointestinal tract (GIT), invariably resulting in incomplete drug absorption, and submaximal therapeutic response (3).…”

Segmental-Dependent Drug Absorption and Delivery: The Stomach

“…Even though some of these polymers are effective at producing bioadhesion, it is diffi cult to maintain its effectivity because of the rapid turnover of mucus in the GIT and the hydration of the stomach content [ 55 , 56 ]. In spite of that, Singh et al were recently able to develop an effervescent fl oating-bioadhesive formulation that was able to retain the antiviral drug lamivudine for at least 5 h and possessed adequate drug release control and pharmacokinetic extension of plasma levels [ 57 ].…”