Nanometric Biopolymer Devices for Oral Delivery of Macromolecules with Clinical Significance

Abstract Despite commercial production of nonimmunogenic macromolecules, their formulation and optimum delivery still remain as the biggest challenges to pharmaceutical scientists. The poor permeability characteristics through various mucosal membranes due to their large molecular weight and size have been the major concerns for successful delivery of macromolecules. The denaturation with consequent loss in biological activity of macromolecules during dosage form design and gastrointestinal passages have compelled the scientists to search for alternative methods for the design of delivery devices. The most important consideration in designing an effective delivery system is to achieve predictable and reproducible absorption of macromolecules into systemic circulation with high bioavailability. Despite enormous gastrointestinal tract (GIT) barriers, peroral route of administration can be very well appreciated from obvious advantages, such as ease of administration and large patient acceptability. Recently, biopolymers have gained popularity because of their nontoxicity, biodegradability, and biocompatibility in designing drug delivery systems either in their native or chemically modified forms. A plethora of reports is available on the preparation of biopolymer-based nanoparticles for the oral delivery of macromolecules, such as protein/peptide, vaccines, gene and enzymes. The purpose of this chapter is to discuss various biological and physicochemical barriers, strategies adopted in augmenting bioabsorption of macromolecules and the mechanisms behind their oral transport. The special emphasis is given to the recent developments in the area of nanobiopolymer devices for effective delivery of macromolecules.