Published January 1, 2013 | Version v1
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Niosomes encapsulating paclitaxel for oral bioavailability enhancement: preparation, characterization, pharmacokinetics and biodistribution

  • 1. Ankara Univ, Fac Pharm, Dept Pharmaceut Technol, TR-06100 Ankara, Turkey
  • 2. Ankara Univ, Fac Pharm, Dept Pharmacol, TR-06100 Ankara, Turkey
  • 3. Ankara Univ, Fac Engn, Dept Chem Engn, TR-06100 Ankara, Turkey

Description

In this study, niosome formulations were prepared and evaluated for their effects on improving the oral bioavailability of paclitaxel (PCT). Niosomes were prepared from Span 40 and coated with bioadhesive carbopol polymers. The niosomes encapsulated 98.7% +/- 0.8 of the initially added PCT and their size ranged from 133 +/- 6 nm to 320 +/- 6 nm. The stability of Carbopol 974P coated niosomes in bile salts was better than uncoated niosomes. Extended release of PCT was observed. After oral administration of formulations to Wistar rats, higher drug plasma concentrations were observed for niosomes comparing to PCT suspension. The high PCT accumulation in intestine and liver obtained after Carbopol 974P coated niosomes administration indicated their potential regarding effective treatment of localized carcinomas in intestine and liver. The relative bioavailability of PCT was increased 3.8- and 1.4-fold by uncoated and Carbopol 974P coated niosomes emphasizing the ability of niosomes on improving the oral bioavailability of PCT.

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