FACTORS INFLUENCING RECTAL DRUG DELIVERY USING NATURAL TERPENES

*Prof. Heyam Saad Ali and Dr. Babiker MA El-Haj

ABSTRACT

Introduction: Diclophenac Sodium DCS is a non-steroidal drug known to be subject to first pass effect after oral administration. The aim of this study was to prepare and evaluate DCS suppositories. To investigate the ability of bisabolol Terpenes to improve drug release compared to other factors. Method: Suppositories were prepared by a fusion method using different fatty bases, viz., Suppocire AS2, and Cocoa butter, as well as different hydrophilic bases, viz. polyethylene glycol and mixture of PEG bases. Terpenes are reported to significantly enhance the cumulative release amount of drug at its low concentration comparing with other synthetic penetration enhancers, and could play an important role in rectal delivery. Chamomile oil contains Bisabolol terpene and has antimicrobial and low toxic and side effects if compared with surfactants. Visual, physical evaluation and In vitro release studies were conducted to different plain based suppositories with or without chamomile or surfactants. Results: Results revealed a greater release of the drug from fatty bases than from hydrophilic bases. Regarding the effect of incorporating Chamomile oil, different types and concentrations of non-ionic surfactants (Tween 40 and Span 80) on the release rate of the drug, it was found that Suppocire AS2 based suppositories with Chamomile oil and 0.5% Tween 40 achieved a very fast 95% drug release at 30 mins. Conclusion: In conclusion, Suppocire As2 based suppositories is selected with Chamomile oil and 0.5% Tween 40 to be suitable for fast release of the drug for immediate release rectal applications of Diclophenac Sodium. Hence, they appear to offer further research and it is great promise for clinical trials and use in suppositories formulations.

Keywords: fatty bases, viz., Suppocire AS2, and Cocoa butter.