Development and in vitro evaluation of surfactant systems for controlled release of zidovudine

The development of a controlled‐release dosage form of zidovudine (AZT) is of crucial importance, in view of the pharmacokinetics of its toxic activity. A suitable drug delivery system could increase AZT bioavailability, reducing its dose‐dependent side effects. In this study, systems composed of po...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2010-05, Vol.99 (5), p.2367-2374
Main Authors: Carvalho, Flávia C., Sarmento, Victor H.V., Chiavacci, Leila A., Barbi, Mariana S., Gremião, Maria P.D.
Format: Article
Language:English
Subjects:
Anti-HIV Agents - administration & dosage
Anti-HIV Agents - pharmacokinetics
Biological and medical sciences
controlled release
Delayed-Action Preparations
dissolution
Drug Carriers - chemistry
Drug Compounding
Fatty Alcohols - chemistry
formulation vehicle
General pharmacology
mathematical model
Medical sciences
microemulsion
Oleic Acid - chemistry
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyethylene Glycols - chemistry
Polymers - chemistry
Propylene Glycols - chemistry
Rheology
Scattering, Small Angle
Solubility
Surface-Active Agents - chemistry
surfactants
X-Ray Diffraction
Zidovudine - administration & dosage
Zidovudine - pharmacokinetics
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Summary:The development of a controlled‐release dosage form of zidovudine (AZT) is of crucial importance, in view of the pharmacokinetics of its toxic activity. A suitable drug delivery system could increase AZT bioavailability, reducing its dose‐dependent side effects. In this study, systems composed of polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol as surfactant (S), oleic acid as oil phase (O), and water (W) were developed, as possible AZT control release systems. They were characterized by polarized light microscopy (PLM), SAXS, and rheological analysis, followed by in vitro release assay. PLM and SAXS results indicated that the mixtures of S/O/W in the proportions 55/35/10 and 55/25/20 formed microemulsion (ME) systems, while 55/20/25 formed lamellar phase. The incorporation of AZT in these systems was greater than in water or oil; moreover, AZT incorporation did not significantly change the phase behavior of the mixtures. MEs behave as Newtonian fluids in flow rheological analysis and the lamellar phase as a pseudoplastic fluid. The release profile indicated that AZT could be released in a controlled manner, since an exponential pattern governs AZT diffusion, as demonstrated by the Weibull mathematical model. These systems are potential carriers for AZT and could have advantages over conventional pharmaceutical forms. © 2009 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 2367–2374, 2010
ISSN:0022-3549
1520-6017
1520-6017
DOI:10.1002/jps.22005