Abstract
Gastrointestinal absorption remains indispensable in the systemic delivery of most drugs, even though it presents several challenges that, paradoxically, may also provide opportunities that can be exploited to achieve maximal bioavailability. Drug delivery systems made from nanoparticle carriers and especially, lipid carriers, have the potential to traverse gastrointestinal barriers and deploy in the lymphatic pathway, which aptly, is free from first pass via the liver. Several poorly soluble drugs have presented improved systemic bioavailability when couriered in lipid nanoparticle carriers. In this review, we propose an additional frontier to enhancing the bioavailability of poorly soluble drugs when encapsulated in lipid nano-carriers by imparting muco-adhesion to the particles through application of appropriate polymeric coating to the lipid carrier. The combined effect of gastrointestinal muco-adhesion followed by lymphatic absorption is a promising approach to improving systemic bioavailability of poorly soluble drugs following oral administration. Evidence to the potential of this approach is backed-up by recent studies within the review.
Highlights
Gastrointestinal absorption remains indispensable in the systemic delivery of most drugs, even though it presents several challenges that, paradoxically, may provide opportunities that can be exploited to achieve maximal bioavailability
The effect of food on gastrointestinal physiology, including altered gastric emptying times of dosage forms and physical interaction between the active pharmaceutical ingredients (API) and the food play a role in how much is presented at the target site
Apart from the effect of food on gastric emptying of dosage forms, food can alter the pharmacokinetics of APIs indirectly by interacting with gut-wall metabolizing enzymes
Summary
The oral route of administration remains most popular among patients because it is the most natural way to get medicines into the body. Nanoparticles can serve as drug delivery carriers for meshwork formed from theofmacromolecules creates random with size the gastrointestinal absorption poorly soluble APIs [16,17,18]. Inpores, this regard, it isindesirable order of nm, which serves as a conduit for the delivery of submicron particles. Nanoparticles with adequate surface charge can be used to cargo poorly soluble APIs across the epithelia for improved systemic bioavailability In this regard, lipid-based carriers such as solid lipid nanoparticles (SLN) or nanostructured lipid carriers (NLC) have a prime advantage for being lipidic and following a lymphatic trajectory whilst avoiding the first pass via the liver [20,21]. We present an observation from the literature that points to the proposition of utilizing a combined approach of nano-formulation through lipid carrier systems and muco-adhesion as a rational approach to improving bioavailability of APIs destined for gastrointestinal absorption
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