The Sojourn from Parenteral to Oral Taxanes using Nanocarrier Systems: A Patent Review.

The Sojourn from Parenteral to Oral Taxanes using Nanocarrier Systems: A Patent Review. Recent Pat Drug Deliv Formul. 2015 Oct 2; Authors: Khurana RK, Teenu, Mahajan M, Kapoor S, Jain S, Singh B Abstract Natural diterpenoid taxanes and their semisynthetic analogues have already made an indelible mark in the chemotherapeutic world for treating various kinds of malignancies. However, due to the absence of any functional groups which could be ionized by pH alteration or which may participate in salt formation, these taxanes, exhibit low solubility. Parenteral administration of taxanes with solubilising agents such as Cremophor EL and Polysorbate 80 results in undesirable side effects like hypersensitivity reactions, myelosuppression and peripheral neuropathy. Nanoengineered drug delivery systems like nanoemulsions, nanocrystals, dendrimers, micelles, self-nanoemulsifying systems, liposomes, solid-lipid nanoparticles and biodegradable polymeric nanoparticles, in this regard, tend to surmount these ostensible challenges, when administered orally. The bare taxanes encounter several inadequacies, namely poor aqueous solubility, structural instability in physiological fluids, p-glycoprotein recognition, hepatic first-pass effect, gastrointestinal permeability, and Cytochrome P450 enzymatic metabolism, etc. In addition, nanoscaled oral delivery improves drug encapsulation, thus facilitating diffusion through intestinal epithelium, modificatio...
Source: Recent Patents on Drug Delivery and Formulation - Category: Drugs & Pharmacology Tags: Recent Pat Drug Deliv Formul Source Type: research