Drug development and industrial pharmacy · 2026
Preparation, characterization of geraniol/HP-β-CD inclusion complex and its acute toxicity evaluation in mice.
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Pu ZhongHui, Luo SiYi, Liao XingYun, Ning YiXiao, Dai Min
Аннотация
OBJECTIVE: This study prepared a geraniol (Ger)/hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex (IC) and evaluated its acute toxicity in mice to support applications in functional foods and pharmaceuticals..
SIGNIFICANCE: Poor stability and irritation limit Ger use; HP-β-CD complexation improves stability, controls release, and reduces toxicity.
METHODS: Response surface methodology optimized IC preparation, while SEM, XRD and other methods confirmed formation. Thermal stability and in vitro release were tested, and intramuscular acute toxicity in mice determined LD50.
RESULTS: Optimal conditions were 100 mg/mL HP-β-CD, 20% acetonitrile, and 35.6 °C, achieving 73.08% encapsulation efficiency. The IC retained over 80% efficiency after 25 days at 4, 25 and 50 °C and showed sustained release (90% at 8 h vs. 2 h for free Ger). The IC LD50 was 2373.96 mg/kg, higher than 1932.49 mg/kg for free Ger, with no major organ lesions.
CONCLUSION: Ger/HP-β-CD IC exhibits sustained-release properties and better safety than free Ger. It is an effective Ger delivery system and supports its potential development and application in functional foods and drugs.
SIGNIFICANCE: Poor stability and irritation limit Ger use; HP-β-CD complexation improves stability, controls release, and reduces toxicity.
METHODS: Response surface methodology optimized IC preparation, while SEM, XRD and other methods confirmed formation. Thermal stability and in vitro release were tested, and intramuscular acute toxicity in mice determined LD50.
RESULTS: Optimal conditions were 100 mg/mL HP-β-CD, 20% acetonitrile, and 35.6 °C, achieving 73.08% encapsulation efficiency. The IC retained over 80% efficiency after 25 days at 4, 25 and 50 °C and showed sustained release (90% at 8 h vs. 2 h for free Ger). The IC LD50 was 2373.96 mg/kg, higher than 1932.49 mg/kg for free Ger, with no major organ lesions.
CONCLUSION: Ger/HP-β-CD IC exhibits sustained-release properties and better safety than free Ger. It is an effective Ger delivery system and supports its potential development and application in functional foods and drugs.