| DOI: https://doi.org/10.14456/mujps.2016.3 | Pharm Sci Asia 2016; 43(1), 28-36 |
Effect of polymeric micelles on the characteristics and stability of diazepam-loaded hydrophilic and lipophilic suppositories W. Siriratawan, K. Narapanich, A. Tungthanabordee, T. Ratanasawetasak, D. Chantasart, J. Suksiriworapong*
1 Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
2 Center of Excellence in Innovation Drug Delivery and Nanomedicine, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
The polymeric micelles can overcome the poor solubility of drug in physiological fluid. However, the incorporation of polymeric micelles in suppository may affect the characteristics and stability of suppository. The aim of this study was to investigate the effect of diazepam-loaded polymeric micelles (DZ-PM) on the characteristics and stability of hydrophilic and lipophilic rectal suppositories in comparison with DZ powder (DZ-PD). The suppositories containing DZ-PD or DZ-PM equivalent to 5 and 10 mg of DZ were prepared by fusion method using PEG4000:PEG400 and Suppocire® AM:BM at 1:1 weight ratio as hydrophilic and lipophilic suppository bases, respectively. The results revealed that the incorporation of DZ-PM had no effect on the uniformity of mass and melting range of all formulations as compared to those containing DZ-PD. In addition, the DZ-PM did not affect the dissolution behaviors of hydrophilic suppository (>80% within 45 min). Meanwhile, the micelles dramatically enhanced the dissolution efficiency of DZ from the lipophilic suppository by at least 5.5 times and reduced the mean dissolution time by 2.0 times as compared to DZ-PD. After stored at 2-8°C for 180 days, the appearance, uniformity of mass, %drug content and dissolution behaviors of all formulations remained unchanged with respect to the initial time. All formulations remained the %weight deviation less than 5% and the %drug remaining was in the range of 93.66-103.06%. It can be concluded that the DZ-PM significantly enhanced the dissolution of drug from lipophilic suppository but slightly affected the properties of hydrophilic suppository.
Keyword:
Diazepam, Hydrophilic, Lipophilic, Polymeric micelles, Suppository
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