Preparation And Characterization Of Nevirapine Oral Nanosuspensions

1045 words - 5 pages

The objective of this study was to prepare and characterize nevirapine nanosuspensions so as to improve the dissolution rate of nevirapine. Nevirapine is a non-nucleoside reverse transcriptase inhibitor of immunodeficiency virus type-1 and it is poorly water-soluble antiretroviral drug. The low solubility of nevirapine can lead to decreased and variable oral bioavailability. Nanosuspension can overcome the oral bioavailability problem of nevirapine. Nevirapine nanosuspensions were prepared using nanoedge method. The suspensions were stabilized using surfactants Lutrol F 127 or Poloxamer 407 and HPMC. The nanosuspension was characterized for particle size, polydispersibility index, crystalline state, particle morphology, in vitro drug release and pharmacokinetics in rats after oral administration. The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability.
Key words: Nanoedge method, Polydispersibility index, AIDS, Nanosuspension, In vitro drug release, Pharmacokinetic study.
Modification and improvement of solubility has been attempted with much success for the development of effective drug formulation[1]. This is especially true for BCS class II drugs. Compounds exhibiting dissolution rate-limited bioavailability are considered class II according to the BCS classification and these compounds have low and variable bioavailability. The solubility of these drug candidates can be enhanced using suitable conventional formulation strategies, which include co-solvents, milling techniques, super critical processing, solid dispersions, including complexation, and precipitation techniques [2]. There still remains an unmet need to equip the pharmaceutical industry with tools to effectively enhance the solubility of BCS class II compounds. With particle engineering technologies, the solubility can be enhanced. Nanosuspension technology is one such technique. With decrease in size, the surface area increases and thereby improved solubility can be achieved. In this regard, nanoscale formulations have attracted attention of various pharmaceutical scientists and these products especially, nanosuspensions, demonstrated clinical and market success [3]. The reduction of drug particles to nanosize leads to a significant increase in the dissolution rate, solubility and therefore enhances bioavailability. Nanosuspensions lead to a reduction in the particle size and/or can transform drugs from a crystalline to an amorphous state and thereby enhance the dissolution rate and solubility [4]. Variability of fed-fasted state bioavailability with nanosuspension formulation can be reduced. Increase in saturation solubility is achieved with nanosuspenions by an increase in dissolution rate of the compound. There is an increase in bioavailability due to increased dissolution rate, solubility as well as increased surface area with nanosuspensions[5]. There can be a greater increase in the bioavailability with...

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