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Sci. Pharm. 2009, 77(1), 123-132; doi:10.3797/scipharm.0803-13

Pharmacokinetic Evaluation of Wheat Germ Agglutinin-Grafted Nanoparticles of Mometasone Furoate

TIFAC-CORE in NDDS, Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The Maharaja Sayajirao University of Baroda, Vadodara 390001, Gujarat, India
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Received: 18 March 2008 / Accepted: 2 December 2008 / Published: 13 December 2008
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Abstract

The aim of the investigation was to assess the pharmacokinetic parameters of wheat germ agglutinin (WGA)-grafted nanoparticles of mometasone furoate (MF), after intratracheal instillation in rats. PLGA (50:50) nanoparticles (NPs) loaded with MF were prepared by emulsion-solvent evaporation technique. WGA was conjugated to spherical MF loaded nanoparticles by carbodiimide coupling yielding a ligand density of 10-15μg WGA / mg NP. The nanoparticles were characterized for size, zeta potential, entrapment efficiency and in-vitro drug release. Plain drug, MF nanoparticles and WGA-grafted MF nanoparticles were administered intratracheally in rats and at different time intervals drug levels in the lung tissue and bronchoalveolar lavage (BAL) were estimated using HPLC. Cumulative MF-release from unconjugated and conjugated MFnanoparticles after 2 weeks was 68% and 55% of the initial drug loading. From the lung MF concentration vs time plot, AUC for WGA-MF-NPs and MF-NPs was found to be 5.9 and 3.8 times higher than AUC for plain MF. This improvement of intracellular drug uptake by means of WGA-conjugation might be due to bioadhesive nature of the lectin which provides an intimate contact to lung mucosal cells followed by facilitated transcytosis as confirmed by improved pharmacokinetic behaviour. All in all, these findings are expected to contribute for better management of asthma to overcome the limitation of short lived action associated with dry powder inhalers.
Keywords: Nanoparticles; Mometasone furoate; Poly[D,L-lactic acid-co-glycolic acid]; Sustained delivery; Wheat germ agglutinin Nanoparticles; Mometasone furoate; Poly[D,L-lactic acid-co-glycolic acid]; Sustained delivery; Wheat germ agglutinin
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

SURTI, N.; NAIK, S.; MISRA, A. Pharmacokinetic Evaluation of Wheat Germ Agglutinin-Grafted Nanoparticles of Mometasone Furoate. Sci. Pharm. 2009, 77, 123-132.

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