A bioactive association platform delivery system for enhanced efficacy of pharmaceutical products

Abstract

Oral delivery of drugs is inundated by formulation challenges predominantly due to poor physicochemical properties of chemical entities resulting in anomalies in serum levels and inconsistent pharmacokinetics and pharmacodynamics. Similar challenges exist for nutraceutical products however, there has been a recent shift in research paradigms towards novel formulation strategies to render these agents invaluable complementary treatments. In this view, vitamin D has gained interest, however it’s effective therapeutic use is limited by low aqueous solubility, erratic inter-patient response, and inadequate formulation design. Cholecalciferol (D3), being a potent form of the vitamin, is widely supplemented and prescribed and was selected as the model agent for proof of concept in the design of a novel oral Drug Delivery System (DDS) in the current research. An ideal physiological milieu is often essential for intended performance of even advanced DDS’s. GIT topology may have an even greater impact on modified dosage forms compared to conventional dosage forms. The use of absorption and solubility enhancers is a tried and tested formulation strategy to improve bioavailability and efficacy of drugs with unfavourable physicochemical characteristics. Despite being an integral part of modern formulation design, these bioenhancers may prove only marginally effective in oral delivery unless the physiological state is considered during formulation. It was therefore imperative that the DDS designed in this investigation included measures to mitigate this effect and achieve robust efficacy regardless of the dynamic GIT condition. In addition, most nutraceuticals typically occur as multicomponent products, yet different combined BCS class vitamins may encounter erratic absorption due to differences in solubility and flocculation effects that impede dispersion in aqueous media. It is therefore imperative to formulate and evaluate a DDS containing more than one nutraceutical agent for greater “real-world” relevance instead of a single vitamin DDS formulation that has been pursued in past studies. The current work therefore set out to develop a DDS capable of orally delivering multiple nutraceutical actives and biological constituents from a single formulation framework with modifiable release kinetics and a unified release of synergistic vitamins, with D3 as the focus agent for enhanced oral bioavailability. Few researchers have investigated the use of multiple biological enhancers combined with synthetic carriers in a dosage form to aid nutraceutical delivery