Co-stabilization of pioglitazone HCL nanoparticles prepared by planetary ball milling: in-vitro and in-vivo evaluation

Pioglitazone (PGZ) is an oral antidiabetic agent that increases cell resistance to insulin, thereby decreasing blood glucose levels. PGZ is a class II drug. Because of its pH-dependent solubility, it precipitates at the intestinal pH, resulting in an erratic and incomplete absorption following oral...

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Bibliographic Details
Published in:Pharmaceutical development and technology 2020-08, Vol.25 (7), p.845-854
Main Authors: Alshora, Doaa H., Alsaif, Shaikha, Ibrahim, Mohamed A., Ezzeldin, Essam, Almeanazel, Osaid T., Abou El Ela, Amal El Sayeh, Ashri, Lubna Y.
Format: Article
Language:eng
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Summary:Pioglitazone (PGZ) is an oral antidiabetic agent that increases cell resistance to insulin, thereby decreasing blood glucose levels. PGZ is a class II drug. Because of its pH-dependent solubility, it precipitates at the intestinal pH, resulting in an erratic and incomplete absorption following oral administration, which causes fluctuations in its plasma concentration. A nanoparticle drug delivery system offers a solution to enhance the dissolution rate of this poorly water-soluble drug. PGZ nanoparticles were formulated by the wet milling technique using a planetary ball mill. The effects of the steric stabilizer (Pluronic F-127, PL F-127), electrostatic stabilizer (sodium deoxycholate, SDC), and number of milling cycles were optimized using a Box-Behnken factorial design. The results showed that the ratio of PL F-127: SDC significantly affected the zeta potential and the dissolution efficiency (DE%) of PGZ. The optimized PGZ nanoparticle formulation enhanced the dissolution to reach 100% after 5 min. The in-vivo results showed significant enhancement in C max (1.3-fold) compared to that of the raw powder, and both AUC 0-24 and AUC 0-∞ were significantly (p 
ISSN:1083-7450
1097-9867