Merck
CN

Oral bioavailability: issues and solutions via nanoformulations.

Clinical pharmacokinetics (2015-02-11)
Kamla Pathak, Smita Raghuvanshi
ABSTRACT

The delivery of drugs through the oral route is regarded as most optimal to achieve desired therapeutic effects and patient compliance. However, poor pharmacokinetic profiles of oral drug candidates remains an area of concern, and approaches to enhance their bioavailability are widely cited in the literature. Traditionally, the approaches have been confined to molecular optimization of the drug molecule, which has gradually evolved into development of microsized and nanosized formulations. Nanoformulations, by virtue of their nanosize, are widely acclaimed for circumventing the obstacles of poor pharmacokinetics. In this review, an attempt has been made to discuss existing challenges of bioavailability and approaches to overcome the same, with in-depth compilation of the literature on nanoformulations. The nanoformulations reviewed include nanocrystals, nanoemulsions, polymeric nanoparticles, self-nanoemulsifying drug delivery systems, dendrimers, carbon nanotubes, polymeric micelles and lipid nanocarriers. This review confirms the potential of nanomedicines to improve the pharmacokinetics of drugs via nanoformulations. Chemotherapeutic applications and patent reports are also compiled in the review. Despite the promising benefits, nanomedicines are associated with hazards to human health. Hence, the review also deals with toxicological consequences of nanomedicines, and with in vitro/in vivo screening methods to assess bioavailability as per regulatory considerations. Nanotechnology has been shown to facilitate the clinical translation of drug candidates that were deemed to be bioavailability failures. Conclusively, nanotechnological approaches to particle design and formulation are beginning to expand the market for many drugs with improved bioavailability and therapeutics. However, dedicated efforts are needed to develop advanced nanomedicines with minimal or no adverse effects.

MATERIALS
Product Number
Brand
Product Description

Supelco
Quercetin, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Quercetin, ≥95% (HPLC), solid
USP
Quercetin, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Oleic acid, meets analytical specification of Ph, Eur., 65.0-88.0% (GC)
Supelco
Oleic acid, analytical standard
Sigma-Aldrich
Oleic acid, technical grade, 90%
Supelco
Oleic acid, Selectophore, ≥99%
Sigma-Aldrich
Oleic acid, natural, FCC
Sigma-Aldrich
Oleic acid, ≥99% (GC)
Sigma-Aldrich
Oleic acid, suitable for cell culture, BioReagent
Oleic acid, European Pharmacopoeia (EP) Reference Standard