伊维菌素纳米乳透皮制剂的研究

doi:10.16431/j.cnki.1671-7236.2015.02.026

Abstract

Abstract: The aim of the study was to prepare ivermectin nanoemulsion for transdermal drug delivery.The physicochemical property,stability,in vitro drug release and transdermal property were evaluated.The optimal drug loading with good stability and larger nanoemulsion region was investigated by ternary phase diagram.The response surface methodology was used for selecting the optimal prescription.The average diameter,zeta potential,morphology,pH and viscosity were also investigated.In vitro drug release and transdermal property of ivermectin nanoemulsion and market ivermectin skin varnish were compared by dialysis bags and Franz diffusion cells.The nanoemulsion region was largest and most stable when the drug loading was 2.00%.The optimal prescription was Cremophor EL-35 :Transcutol HP :ethyl oleate :ivermectin :H₂O=26: 12: 7: 2: 53 and its average diameter was 18 nm.The ivermection nanoemulsion was stable when it was stored in 4 ℃ refrigerator and room temperature for 1 year.The cumulative permeation and retention of ivermectin nanoemulsion in 24 h were 3.24 and 2.05 times over the commercially available varnish,respectively.These results indicated that the ivermectin nanoemulsion had the advantages of simple preparation process,excellent stability and transdermal property,and had good application prospects.

Key words: ivermectin; nanoemulsion; ternary phase diagram; response surface methodology; in vitro drug release; transdermal property

CLC Number:

S859.7

DING Dan, SHENG Xiao-li, LIANG Kong-xian, XU Qi, LIU Wei. Study on Ivermectin Nanoemulsion for Transdermal Drug Delivery[J]. , 2015, 42(2): 401-407.

References

[1] Chhaiya S B,Mehta D S,Kataria B C.Ivermectin:Pharmacology and therapeutic applications[J].International Journal of Basic & Clinical Pharmacology,2012,1(3):132-139.
[2] Shakeel F,Baboota S,Ahuja A.Celecoxib nanoemulsion for transdermal drug delivery:Characterization and in vitro evaluation[J].Journal of Dispersion Science and Technology,2009,30(6):834-842.
[3] Shafiq S,Shakeel F,Talegaonkar S.Development and bioavailability assessment of ramipril nanoemulsion formulation[J].European Journal of Pharmaceutics and Biopharmaceutics,2007,66(2):227-243.
[4] Shakeel F,Shafiq S,Haq N.Nanoemulsions as potential vehicles for transdermal and dermal delivery of hydrophobic compounds[J].Informa Healthcare,2012,9(8):953-974.
[5] 汪杨,吴伟,阙俐.油-吐温-醇-水体系伪三元相图在自微乳乳化制剂研究中的应用[J].中国医药工业杂志,2005,36(6):345-348.
[6] 陈玲,周建平.微乳的处方因素对伊维菌素体外透皮性能的影响[J].中国药学杂志,2006,41(15):1154-1157.
[7] Zhou H,Wan J L,Wu L,et al.A new strategy for enhancing the oral bioavailability of drugs with poor water solubility and low liposolubility based on phospholipid complex and supersaturated SEDDS[J].PLoS One,2013,8(12):e84530.
[8] Dixit N,Kohli K,Baboota S.Nanoemulsion system for the transdermal delivery of a poorly soluble cardiovascular drug[J].PDA Journal of Pharmaceutical Science and Technology,2008,62(1):46-55.
[9] 姚新武,刘长霞,张鹏.响应面法优化龙胆苦苷脂质体的复乳法制备工艺[J].北京化工大学学报(自然科学版),2012,39(2):68-73.
[10] Tsai Y H,Fu L T,Huang C T,et al.Formulation optimization of estradiol microemulsion using response surface methodology[J]. Journal of Pharmaceutical Sciences,2011,100(10):4383-4389.
[11] 刘根新,张继瑜,吴培星,等.伊维菌素纳米乳注射液的研制与质量安全性评价[J].畜牧兽医学报,2011,42(8):1161-1167.
[12] 何书海,巴桑旺堆,佘永新.伊维菌素小单室脂质体工艺配方优化及质量分析[J].中国畜牧兽医,2012,39(7):108-112.
[13] Chen S Y,Liu W,Wan J L,et al.Preparation of coenzyme Q10 nanostructured lipid carriers for epidermal targeting with high pressure microfluidics technique[J].Drug Development and Industrial Pharmacy,2013,39(1):21-28.
[14] Hathout R M,Woodman T J,Mansour S,et al.Microemulsion formulations for the transdermal delivery of testosterone[J]. European Journal of Pharmaceutical Sciences,2010,40(3):188-196.
[15] Sintov A C,Shapiro L.New microemulsion vehicle facilitates percutaneous penetration in vitro and cutaneous drug bioavailability in vivo[J].Journal of Controlled Release,2004,95(2):173-183.
[16] Azeem A,Ahmad F J,Khar R K,et al.Nanocarrier for the transdermal delivery of an antiparkinsonian drug[J].AAPS Pharmaceutical Science and Technology,2009,10(4):1093-1103.
[17] Rizwan M,Aqil M,Azeem A,et al.Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle[J].Journal of Experimental Nanoscience,2010,5(5):390-411.

Study on Ivermectin Nanoemulsion for Transdermal Drug Delivery

Knowledge

Abstract

Cite this article

share this article

References

Related Articles 15

Recommended Articles

Metrics

Comments

[1]	SUN Yuanyuan, LIANG Chuncai, ZHANG Hailong, LIU Juxiang. Preparation of Hydrogel Drug Carrier for Chicks [J]. China Animal Husbandry and Veterinary Medicine, 2022, 49(10): 4075-4084.
[2]	XU Baichang, FANG Ziyi, MENG Jinyan, CUI Qinghan, LI Hongman, SI Hongbin. Optimization of Extraction Process and Antioxidant Activity of Polyphenols from Leaves of Broussonetia papyrifera [J]. China Animal Husbandry and Veterinary Medicine, 2021, 48(3): 1046-1053.
[3]	WU Xinyu, YAN Lin, WU Hong. Optimizing Conditions Analysis of Levan by Whole-cell Biocatalysis with Corynebacterium glutamicum [J]. China Animal Husbandry and Veterinary Medicine, 2020, 47(11): 3474-3483.
[4]	LIU Yingying, YUE Zhiguang, WU Ningpeng, LIU Zhenzhen, YAN Yaqun, ZHANG Sumei, JIAN Fuchun, ZHANG Longxian, WANG Rongjun, NING Changshen. Comparative Study on Pharmacokinetics of Long-acting Transdermal Agents of Ivermectin and Common Injection in Rabbits [J]. China Animal Husbandry and Veterinary Medicine, 2020, 47(1): 267-274.
[5]	SHI Feifei, WANG Jing, QIN Feng, CHEN Xiaolan, GAO Jianru, WEI Yu, ZHANG Long. Study on Pharmacokinetics of a Novel Veterinary Nanoemulsion Drug Loading System in Rats [J]. , 2019, 46(4): 1236-1243.
[6]	CHEN Keyuan, HAO Baocheng, DING Ziqiang, LIANG Jianping. Optimization of Liquid Fermentation Process for Danggui Buxue Tang by Response Surface Methodology [J]. China Animal Husbandry and Veterinary Medicine, 2019, 46(10): 2946-2954.
[7]	WANG Si-han, ZHANG Ji-yu, XING Shou-ye, LI Bing, ZHOU Xu-zheng. Content Determination of Ivermectin in the Ivermectin Microemulsion Injection [J]. , 2017, 44(6): 1861-1868.
[8]	TIAN Qi-zhen, CAI Bing-yan, YUAN Wei-feng. Efficacy of Chinese Herbal Medicine Canine Acariasis Spirit on Demodex canis [J]. , 2017, 44(11): 3358-3364.
[9]	XING Shou-ye, ZHOU Xu-zheng, LI Bing, NIU Jian-rong, WEI Xiao-juan, ZHANG Ji-yu. Study on Sterility Test Method of Ivermectin Microemulsion [J]. , 2016, 43(1): 256-260.
[10]	XING Shou-ye, ZHOU Xu-zheng, LI Bing, NIU Jian-rong, WEI Xiao-juan, ZHANG Ji-yu. Allergic Study of Ivermectin Microemulsion [J]. , 2014, 41(11): 275-278.
[11]	HE Shu-hai, BASANG Wang-dui, SHE Yong-xin. Optimizing Process and Formula and Analyzing Quality for Ivermectin Single Unilamellar Vesicles [J]. , 2012, 39(7): 108-112.
[12]	ZHANG Rui-li;CUI Liang-Liang;HAO Zhi-hui;ZHAO Yong-da. Compare Pharmacokinetics of 5 Different Ivermectin Injection in Rabbit [J]. , 2011, 38(11): 188-190.
[13]	JIANG Xiao-wen;ZHANG Chun-yan;YU Wen-hui;XU Li. Study on Pharmacokinetics of Ivermectin Emulsion Compound in Goats [J]. , 2010, 37(8): 169-171.
[14]	JIANG Xiao-wen;FENG Guo-feng;XU Ming-xing. Effects of Ivermectin on Male Rats Procreation [J]. , 2010, 37(6): 174-175.
[15]	SHE Yong-xin;Badsang wangdui;SE Zhu;HE Shu-hai;WANG Jing;DONG Lu-de;Laba cidan;YANG De-quan. Determination of Content and Entrapment Efficiency for Ivermectin Liposomes by HPLC [J]. , 2010, 37(4): 80-84.