Extraction and Microencapsulation of Khat: Effects on Sexual Motivation and Estradiol Level in Female Rats

Abstract

Introduction Khat (Catha edulis) is an evergreen tree/shrub that is thought to affect sexual motivation or libido. Its positive effect on sexual desire is more frequently observed in females than in males and occurs when khat is chewed. Thus, khat’s effects on sexual behavior may depend on the release mode of its active constituent. Aim This study aimed to investigate the effect of dried khat alkaloids on the sexual motivation and estradiol levels of female rats, with special emphasis on the importance of the sustained release effect. Methods Dried khat leaves were extracted and isolated. The alkaloids in khat extract were identified and calculated using thin layer chromatography and high-performance liquid chromatography. The isolated khat extract was microencapsulated using a phase separation coacervation method. The morphology, particle size, yield, drug loading, and entrapment efficiency were evaluated. The in vitro release and stability of alkaloids in khat extract and in khat extract microcapsules were determined. The effect of khat extract microcapsules and varying doses of khat extract on sexual motivation in female rats were investigated. Additionally, estradiol levels, vaginal secretions and vaginal pH were determined. Main Outcome Measures The differences in the effect of khat extract and khat extract microcapsules on sexual motivation, vaginal secretion and estradiol levels in female rats were compared. Results Cathine and norephedrine were identified in the isolated khat extract at composition of 81.3% and 17.2%, respectively. Among the formulations studied, khat extract microcapsules of formulation 2:3:5 (containing a ratio of khat extract to ovalbumin to gelatin of 2:3:5) were found to exhibit higher yield, loading, and entrapment efficiency. Khat extract microcapsules showed sustained in vitro release and were more stable than khat extract. In addition, khat extract microcapsules enhanced sexual motivation, increased vaginal secretions, and upregulated estradiol level in female rats. Conclusion The sustained release of alkaloids from dried khat has significantly enhanced the sexual motivation and increased the estradiol level of female rats. Thus the release of dried khat alkaloids from microcapsules might be an effective means of enhancing the libido in females.

Khat (Catha edulis) alters the phenotype and anti-microbial activity of peripheral blood mononuclear cells

“…Typically, 100 g of dried leaves yielded 8 g of khat extract powder. As previously described, high performance liquid chromatography analysis confirmed that alkaloids in the khat extract consisted of 80% cathine and 20% norephedrine; no cathinone was detected (Aziz et al, 2009;Banjaw and Schmidt, 2005;Dimba et al, 2004).…”

“…Khat was extracted from leaves as described previously (Aziz et al, 2009;Banjaw and Schmidt, 2005;Dimba et al, 2004). Briefly, dried khat leaves (100 g) were chopped into small pieces, homogenized in 100 mL of 95% ethanol, centrifuged at 5000 rpm for 5 min and the supernatant then filtered with Whatman filter paper (no.…”

Khat (Catha edulis) generates reactive oxygen species and promotes hepatic cell apoptosis via MAPK activation

“…Typically, 100 g of dried leaves yielded 8 g of khat extract powder. As previously described, high performance liquid chromatography analysis confirmed that the alkaloids in the khat extract consisted of 80% cathine and 20% norephedrine; no cathinone was detected (14,21,22). Lyophilized khat extract was dissolved in Hank's buffered salt solution (HBSS) without Ca 2+ , Mg 2+ to a final concentration of 200 µg/ml and filter (0.2 µm) sterilized before being added to the cells.…”

“…After drying, the plant was weighed, packed in a closed foil packet and stored at 4˚C until use. Khat was extracted from the leaves as described previously (14,21,22). Briefly, dried khat leaves (100 g) were swiftly chopped into small (5 mm) pieces and dissolved in 100 ml of 95% ethanol, centrifuged at 5,000 rpm for 5 min and the supernatant then filtered with Whatman filter paper.…”

Adverse Health Effects of Khat: A Review

“…Khat extract enhanced sexual motivation, increased vaginal secretions and up-regulated estradiol level in female rats [48].…”