Micronization of Thebaine Extracted from Papaver Bracteatum Lindl. Using Supercritical Fluid Technology

Abstract

Abstract Background Thebaine, as a main opiate alkaloid extracted from papaveraceae plants, is widely used in the synthesis of many pharmaceutical ingredients such as buprenorphine, naltrexone, naloxone, and hydrocodone. Nevertheless, thebaine and related derivatives are often insoluble in aqueous media and have low bioavailability in digestive system. Objective Reducing particle size and changing the morphology can mitigate the mentioned problem. In this study, extraction of thebaine from the capsule, steam, and root of Papaver bracteatum L. was optimized and micronization of extract components was developed to study of solubility. Methods Extraction process was performed using supercritical carbon dioxide. Experimental central composite design was employed to determine the optimal conditions. Analysis of extract was done using validated HPLC method and mass spectrometry. Micronization process was performed using an inhouse developed supercritical technique. The nanoparticles were characterized using FESEM and Image J software. The Effect of micronization was explored on the solubility of extract components via ultraviolet spectroscopy. Results The percentage of thebaine in dried capsule, steam, and root powder was about 1.05%, 0.31, and 0.83% respectively. The extraction results indicated that supercritical pressure has the greatest effect on the extraction yield. Analysis of FESEM images revealed that nanoparticles of extract components with particle size distribution of 5 to 100 nm were collected successfully. Conclusions The extraction results indicated that pressure has the greatest effect on the extraction yield. In vitro studies illustrated that the solubility of extract components increased up to 1.7 times during the micronization process. Highlights Expansion of supercritical methods as an effective method was performed for extracting and preparing alkaloids nanoparticles. This process led to improved oral bioavailability of alkaloids.