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. 2014 Apr;22(2):133-40.
doi: 10.1016/j.jsps.2013.04.002. Epub 2013 May 3.

Formulation and optimization of coated PLGA - Zidovudine nanoparticles using factorial design and in vitro in vivo evaluations to determine brain targeting efficiency

G V Peter Christoper  1 , C Vijaya Raghavan  1 , K Siddharth  1 , M Siva Selva Kumar  2 , R Hari Prasad  2
Affiliations

Formulation and optimization of coated PLGA - Zidovudine nanoparticles using factorial design and in vitro in vivo evaluations to determine brain targeting efficiency

G V Peter Christoper et al. Saudi Pharm J. 2014 Apr.

Abstract

In the current study zidovudine loaded PLGA nanoparticles were prepared, coated and further investigated for its effectiveness in brain targeting. IR and DSC studies were performed to determine the interaction between excipients used and to find out the nature of drug in the formulation. Formulations were prepared by adopting 2(3) factorial designs to evaluate the effects of process and formulation variables. The prepared formulations were subjected for in vitro and in vivo evaluations. In vitro evaluations showed particle size below 100 nm, entrapment efficiency of formulations ranges of 28-57%, process yield of 60-76% was achieved and drug release for the formulations were in the range of 50-85%. The drug release from the formulations was found to follow Higuchi release pattern, n-value obtained after Korsemeyer plot was in the range of 0.56-0.78. In vivo evaluations were performed in mice after intraperitoneal administration of zidovudine drug solution, uncoated and coated formulation. Formulation when coated with Tween 80 achieved a higher concentration in the brain than that of the drug in solution and of the uncoated formulation. Stability studies indicated that there was no degradation of the drug in the formulation after 90 days of preparation when stored in refrigerated condition.

Keywords: Brain targeting; Coated nanoparticles; Factorial design; Tween 80; Zidovudine.

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Figures

Figure 1
Figure 1
DSC Thermograms of (A) zidovudine and (B) formulation F9.
Figure 2
Figure 2
Surface plot illustrating the influence of PLGA and Poloxamer on particle size of the prepared formulations.
Figure 3
Figure 3
TEM image of tween 80 coated formulation F9.
Figure 4
Figure 4
Surface plot depicting the influence of PLGA and aqueous medium on entrapment efficiency of PLGA nanoparticles.
Figure 5
Figure 5
Cumulative mean % release of zidovudine from PLGA nanoparticles containing poloxamer 407 in PBS pH 7.4.
Figure 6
Figure 6
Surface plot depicting the influence of PLGA and poloxamer on drug release from PLGA nanoparticles.
Figure 7
Figure 7
Concentration of zidovudine (ng/ml) in various organs on administration of the drug solution, F6 and F9.
None
See this image and copyright information in PMC

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