With the advent of novel vesicular drug delivery systems especially bilosomes, for large molecular
weight proteins and peptides, their oral administration seems a viable approach. These nano-vesicles have shown
promising results for the effective delivery of insulin and other therapeutics, perhaps due to their structural composition.
The present review has elaborated the biopharmaceutical challenges for the oral delivery of therapeutic
proteins and peptides as well as presented a novel approach to deliver the essential macromolecules through oral
route as bilosomes. The extensive search has been presented related to the formulation, evaluation and in vivo
performance of bilosomes. Some of the crucial findings related to bilosomes have corroborated them superior to
other colloidal carriers. The successful drug delivery through bilosomes requires significant justifications related
to their interaction with the biological membranes. The other aspects such as absolute absorption, safety and
toxicity of bilosome drug delivery should also be equally considered.
Keywords: Biopharmaceuticals, bilosomes, proteins and peptides, oral delivery, lymphatic transport.
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