两性霉素B阴道用纳米泡沫剂的制备及评价

张星贤, 侯玉婷, 曹杰, 柯学

中国药学杂志 ›› 2019, Vol. 54 ›› Issue (13) : 1078-1085.

PDF(3718 KB)
PDF(3718 KB)
中国药学杂志 ›› 2019, Vol. 54 ›› Issue (13) : 1078-1085. DOI: 10.11669/cpj.2019.13.008
论著

两性霉素B阴道用纳米泡沫剂的制备及评价

  • 张星贤, 侯玉婷, 曹杰, 柯学*
作者信息 +

Preparation and Evaluation of Amphotericin B Vaginal Nanosuspension Foam

  • ZHANG Xing-xian, HOU Yu-ting, CAO Jie, KE Xue*
Author information +
文章历史 +

摘要

目的 制备两性霉素B 阴道用纳米泡沫剂并进行基本理化性质和体内药效学评价。方法 采用单因素法,分别优化处方中的蛋黄磷脂用量和起泡剂参数,制备两性霉素B纳米泡沫剂;进一步考察制剂的药物粒径、泡沫形态、发泡性能等基本理化性质;构建白假丝酵母菌阴道炎小鼠模型,评价药物对阴道炎症的治疗效果。结果 两性霉素B纳米泡沫剂的优化处方中需在5 mg·mL-1的药物量中加入60 mg·mL-1的蛋黄磷脂和30 mg·mL-1的烷基糖苷APG0810,制剂的药物粒径约240 nm,微泡沫直径约200~400 μm,泡沫半衰期约为43.5 min,对小鼠阴道炎症感染有显著治疗效果。结论 采用磷脂纳米粒和起泡剂制备的两性霉素B纳米泡沫剂基本理化性质和体内治疗效果良好,有望成为具有潜力的治疗外阴阴道白色念珠菌感染的药物新剂型。

Abstract

OBJECTIVE To prepare amphotericin B vaginal nanosuspension foam and study the physicochemical properties and in vivo pharmacodynamics. METHODS Using the single factor method, the concentration of egg lecithin and the technical parameters of foaming agent in formulation were gradually optimized. Then, the physicochemical properties, including drug particle size, appearance of foam and formed capability, were studied. The therapeutic effect on vaginal inflammatory infection was investigated with the mouse model of Candida albicans vaginitis. RESULTS The optimal formulation of amphotericin B nanosuspension foam included 5 mg·mL-1 amphotericin B, 60 mg·mL-1 egg lecithin and 30 mg·mL-1 APG0810. The drug particle size, range of micro-foam diameter and foam half-life were about 240 nm, 200-400 μm and 43.5 min, respectively. It was found that amphotericin B nanosuspension vaginal foam had significant therapeutic effect on mouse vaginal inflammation infection. CONCLUSION The amphotericin B nanosuspension foam has good physicochemical properties and excellent pharmacological activity in vivo, which shows potential use for the therapy of vulvovaginal candidiasis.

关键词

两性霉素B / 纳米 / 泡沫剂 / 外阴阴道假丝酵母菌病

Key words

amphotericin B / nanometer / foam / vulvovaginal candidiasis

引用本文

导出引用
张星贤, 侯玉婷, 曹杰, 柯学. 两性霉素B阴道用纳米泡沫剂的制备及评价[J]. 中国药学杂志, 2019, 54(13): 1078-1085 https://doi.org/10.11669/cpj.2019.13.008
ZHANG Xing-xian, HOU Yu-ting, CAO Jie, KE Xue. Preparation and Evaluation of Amphotericin B Vaginal Nanosuspension Foam[J]. Chinese Pharmaceutical Journal, 2019, 54(13): 1078-1085 https://doi.org/10.11669/cpj.2019.13.008
中图分类号: R944   

参考文献

[1] GONÇALVES B, FERREIRA C, ALVES C T, et al. Vulvovaginal candidiasis: epidemiology, microbiology and risk factors [J]. Crit Rev Microbiol, 2015, 42(6):905-927.
[2] LI L, SU T L, MIAO C, et al. To investigate the resistance of Candida albicans to common antifungals drugs [J]. Chin J Lab Diagn (中国实验诊断学), 2011, 15(1):126-128.
[3] HAO X H, MA C. Distribution and resistance analysis of 128 strains of Candida albicans [J]. J Nav Gen Hosp (海军总医院学报), 2008, 21(2):8-10.
[4] HUO L L, LIU Z H. Effects of amphotericin B on vaginal drug-resistant Candida albicans [J]. Chin J Pract Gynecol Obstet(中国实用妇科与产科杂志), 2016, 32(7):667-670.
[5] LEMKE A, KIDERLEN A F, KAYSER O. Amphotericin B [J]. Appl Microbiol Biot, 2005, 68(2):151-162.
[6] PHILLIPS A J. Treatment of non-albicans Candida vaginitis with amphotericin B vaginal suppositories [J]. Am J Obstet Gynecol, 2005, 192(6):2009-2012.
[7] RICHTER S S, GALASK R P, MESSER S A, et al. Antifungal susceptibilities of Candida species causing vulvovaginitis and epidemiology of recurrent cases [J]. J Clin Microbiol, 2005, 43(5):2155-2162.
[8] VANIC Ž, KALKO-BASNET N. Nanopharmaceuticals for improved topical vaginal therapy: can they deliver? [J]. Eur J Pharm Sci, 2013, 50(1):29-41.
[9] MESSINGER H, AULMANN W, KLEBER M, et al. Investigations on the effects of alkyl polyglucosides on development and fertility[J]. Food Chem Toxicol, 2007, 45(8):1375-1382.
[10] SHEN B, SHEN C, XU L, et al. Research progress on in vitro and in vivo behaviors of poorly soluble Chinese materiamedicananosuspension [J]. Chin J Chin Mater Med (中国中药杂志), 2018, 43(19):3828-3833.
[11] YUAN H, YI J, ZHANG C, et al. Progress in research of preparation technologies and drug-delivery of nanosuspensions [J]. Chin J New Drug (中国新药杂志), 2014, 23(3):297-301.
[12] WANG X F. Studyon foaming agents for foam finishing [D]. Hangzhou: Zhejiang University of Science and Technology, 2016.
[13] ARZHAVITINA A, STECKEL H. Foams for pharmaceutical and cosmetic application[J]. Int J Pharm, 2010, 394(1-2):1-17.
[14] MEI L, CHEN J, YU S, et al. Expansible thermal gelling foam aerosol for vaginal drug delivery [J]. Drug Deliv, 2017, 24(1):1325-1337.
PDF(3718 KB)

Accesses

Citation

Detail

段落导航
相关文章

/