Lipid-based oral multiparticulate formulations – advantages, technological advances and industrial applications

Abstract

Introduction: Lipid-based formulations have emerged as potential dosage forms to harvest effectively the therapeutic benefits of existing lipophilic molecules and new chemical entities. Compared with existing excipients, lipids by virtue of their unique physicochemical properties and resemblance to in vivo components demonstrate the extra advantage of improving the bioavailability of lipophilic and highly metabolizable drugs. Moreover, if used as the major excipient, lipids can reduce the required dose and even the toxicity of drugs with poor aqueous solubility.

Areas covered: This review deals with the importance of multiparticulate systems in drug delivery, the therapeutic and manufacturing advantages of lipids as excipients, and the technological advances made so far in utilizing lipids for multiparticulate dosage forms, with emphasis on their application and success on an industrial scale. Lipids are being widely formulated into different multiparticulate dosage forms using innovative modifications of conventional equipment with relative ease, using methods such as melt-granulation, adsorption on solid support, spray-cooling, melt-extrusion/spheronization, freeze-pelletization, pastillation, and so on.

Expert opinion: There is still a need to design new simple dosage forms and to upgrade existing manufacturing technology, in order to open up new avenues in drug delivery, for preparing patent non-infringing formulations of existing drug products, and to help patients receive treatment at an affordable cost.

Keywords::

• drug delivery
• formulation technology
• lipid
• liposomes
• pastillation
• solid lipid nanoparticles
• solid lipid pellets
• solid self-emulsifying drug delivery systems

Notes

This box summarizes key points contained in the article.