Development and optimization of nanoemulsion gel for topical delivery of imiquimod

doi:10.5246/jcps.2018.01.004

中国药学(英文版) ›› 2018, Vol. 27 ›› Issue (1): 31-39.DOI: 10.5246/jcps.2018.01.004

Development and optimization of nanoemulsion gel for topical delivery of imiquimod

Gurvinder Kaur¹, Tanurajvir Kaur², Deepak N. Kapoor^2*

1. School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, India
2. School of Pharmaceutical Sciences, Shoolini University of Biotechnology and Management Sciences, Post Box No.9, Solan-173212, Himachal Pradesh 144411, India

收稿日期:2017-08-19 修回日期:2017-09-20 出版日期:2018-02-28 发布日期:2017-10-15
通讯作者: Tel.: +91-9646142349, E-mail: deepakpharmatech@gmail.com

Development and optimization of nanoemulsion gel for topical delivery of imiquimod

Gurvinder Kaur¹, Tanurajvir Kaur², Deepak N. Kapoor^2*

1. School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, India
2. School of Pharmaceutical Sciences, Shoolini University of Biotechnology and Management Sciences, Post Box No.9, Solan-173212, Himachal Pradesh 144411, India

Received:2017-08-19 Revised:2017-09-20 Online:2018-02-28 Published:2017-10-15
Contact: Tel.: +91-9646142349, E-mail: deepakpharmatech@gmail.com

摘要/Abstract

摘要：

In the present study, we aimed to formulate, optimize and characterize nanoemulsion-based gel of imiquimod for its topical administration and to improve the drug permeation. Nanoemulsions were prepared by the aqueous phase titration method and spontaneously formed by mixing specific fractions of oil phase:S_mix:water. The nanoemulsion formulations were optimized by response surface methodology (RSM) using mixture design, Scheffe model. The formulated nanoemulsion was incorporated into 0.5% Carbopol 934 (w/v) to enhance convenience in superficial application of the drug. The nanoemulsions were characterizedin terms of droplet size, zeta potential, TEM, DSC and in vitro drug permeation. The vesicle size was 113.6 nm with polydispersity index of 0.251. The zeta potential was 34 mV. The spherical droplet shape was confirmed by TEM analysis. The drug permeation from the diffusion membrane was 73.67% in 6 h for the optimized formulation. An optimized nanoemulsion gel formulation of imiquimod was successfully developed with improved permeation using experimental design technique. The developed formulation could be further explored as a potential alternate to currently available topical formulations for the treatment of genital warts.

关键词: Imiquimod, Condyloma acuminata, Human papilloma virus, Genital warts, Nanoemulsions

Abstract:

Key words: Imiquimod, Condyloma acuminata, Human papilloma virus, Genital warts, Nanoemulsions

中图分类号:

R944

Supporting:

Gurvinder Kaur, Tanurajvir Kaur, Deepak N. Kapoor. Development and optimization of nanoemulsion gel for topical delivery of imiquimod[J]. 中国药学(英文版), 2018, 27(1): 31-39.

Gurvinder Kaur, Tanurajvir Kaur, Deepak N. Kapoor. Development and optimization of nanoemulsion gel for topical delivery of imiquimod[J]. Journal of Chinese Pharmaceutical Sciences, 2018, 27(1): 31-39.

参考文献

[1] Shafiq-un-Nabi, S.; Shakeel, F.; Talegaonkar, S.; Ali, J.; Baboota, S.; Ahuja, A.; Khar, R.K.; Ali, M. Formulation Development and Optimization using Nanoemulsion Technique: A Technical Note. AAPS. PharmSciTech. 2007, 8, 1-6.

[2] Azeem, A.; Rizwan, M.; Ahmad, F.Z.; Iqbal, Z.; Khar, R.K.; Aqil, M.; Talegaonkar, S. Nanoemulsion Components Screening and Selection: A Technical Note. AAPS. PharmSciTech. 2009, 10, 69-76.

[3] Debnath, S.; Satayanarayana Kumar, G.V. Nanoemulsion: A Method to Improve the Solubility of Lipophilic Drugs. Int. J. Pharm. Sci. 2011, 2, 72-84.

[4] Devarajan, V.; Ravichandran, V. Nanoemulsions: As Modified Drug Delivery Tool. Int. J. Comp. Pharm. 2011, 2, 1-6.

[5] Maali, A.; Mosavian, M.T.H. Preparation and Application of Nanoemulsions in the Last Decade (2000-2010). J. Disper. Sci. Technol. 2013, 34, 92-105.

[6] Rapose, A. Human PapillomaVirus and Genital Cancer. Ind. J. Derm.Venereol Leprol. 2009, 75, 236-244.

[7] Tchernev, G. Sexually Transmitted Papillomavirus Infections: Epidemiology, Pathogenesis, Clinic, Morphology, Important Differential Diagnostic Aspects, Current Diagnostic and Treatment Options. An. Bras. Derma. 2009, 84, 377-389.

[8] Sharma, S. Vaccines Against Human Papilloma Virus and Cervical Cancer: An Overview. Ind. J. Community Med. 2008, 33, 143-146.

[9] Gall, S.A. Female Genital Warts: Global Trends and Treatments. Inf. Dis. Obs. Gyne. 2001, 9, 149-154.

[10] Kodner, C.M.; Nastraty, S. Management of Genital Warts. Am. Fam. Physician. 2004, 70, 2335-2342.

[11] Tarbet, E.B.; Larson, D.; Anderson, B.J.; Bailey, K.W.; Wong, M.; Smee, D.F. Evaluation of Imiquimod for Topical Treatment of Vaccinia Virus Cutaneous Infections in Immunosuppressed Hairless Mice. Antiviral Res. 2011, 90, 126-133.

[12] Vidal, D.; Alomar, A. Mode of Action and Clinical Use of Imiquimod. Expert Rev Dermatol. 2008, 3, 151-159.

[13] Homhuan, A. Maturation of Dendritic Cells Induced by Nano-liposomes Containing Imiquimod. Asian Biomed. 2008, 2, 233-239.

[14] Lacarrubba, F.; Nasc, M.R.; Micali, G. Advances in the Use of Topical Imiquimod to Treat Dermatologic Disorders. Ther. Clin. Risk Manag. 2008, 4, 87-97.

[15] Lee, W.; Shen, S.; Al-Suwayeh, S.A.; Yang, H.; Yuan, C.; Fang, J. Laser-Assisted Topical Drug Delivery by Using a Low-fluence Fractional Laser: Imiquimod and Macro-molecules. J. Controlled Release. 2011, 153, 240-248.

[16] Tyring, S.K.; Arany, I.; Stanley, M.A.; Tomai, M.A.; Miller, R.L.; Smith, M.H.; Dermott, D.J.; Slade, H.B. A Randomized, Controlled, Molecular Study of Condyloma acuminata Clearance During Treatment with Imiquimod. J. Infect. Dis. 1998, 178, 551-555.

[17] Kapil, R.; Dhawan, S.; Singh, B. Development and Validation of a Spectrofluorimetric Method for the Estimation of Rivastigmine in Formulations. Ind. J. Pharm. Sci. 2009, 71, 581-585.

[18] Kumar, S.H.; Singh, V. J. Nanoemulsification: A Novel Targeted Drug Delivery Tool. Drug Deliv. Ther. 2012, 2, 40-45.

[19] Patel, R.P.; Joshi, J.R. An Overview on Nanoemulsion: A Novel Approach. Int. J. Pharm. Sci. Res. 2012, 3, 4640-4650.

[20] Shakeel, F.; Baboota, S.; Ahuja, A.; Javed, A.; Shafiq, S. Accelerated Stability Testing of Celecoxib Nanoemulsion containing Cremophor-EL. Afri. J. Pharm. Pharmacol. 2008, 2, 179-183.

[21] Gupta, P.K.; Pandit, J.K.; Kumar, A.; Swaroop, P.; Gupta, S. Pharmaceutical Nanotechnology Novel Nanoemulsion-High Energy Emulsification Preparation, Evaluation and Application. Pharm. Res. 2010, 3, 117-138.

[22] Zheng, W.; Zhao, L.; Wei, Y.M.; Ye, Y.; Xiao, S.H. Preparation and In vitro Evaluation of Nanoemulsion System for the Transdermal Delivery of Granisetron Hydrochloride. Chem. Pharm. Bull. 2010, 58, 1015-1019.
[23] Modi, J.D.; Patel, J.K. Nanoemulsion-Based Gel Formulation of Aceclofenac for Topical Delivery. Int. J. Pharm. Sci. Res. 2011, 1, 6-12.

Development and optimization of nanoemulsion gel for topical delivery of imiquimod

Development and optimization of nanoemulsion gel for topical delivery of imiquimod

RichHTML

PDF (PC)

可视化

摘要/Abstract

引用本文

使用本文

参考文献

相关文章 15

编辑推荐

Metrics

本文评价

[1]	雷萌, 王雪源, 苗航, 王佳, 沙思佳, 朱姜, 朱永强. 叶酸靶向聚合物纳米粒共传输紫杉醇和吉西他滨用于乳腺癌的治疗[J]. 中国药学(英文版), 2020, 29(10): 701-710.
[2]	刘曼, 张爽, 李卓越, 王光雪, 王景茹, 张烜. 氧化锌纳米粒的制备与表征[J]. 中国药学(英文版), 2020, 29(9): 617-625.
[3]	周楚杭, 胡新平, 刘琦, 王乐淇, 周远航, 靳尧, 刘艳. 增强抗肿瘤药物肿瘤靶向性递送的叶酸修饰的pH敏感聚合物胶束[J]. 中国药学(英文版), 2020, 29(9): 626-636.
[4]	余飞, 周文莉, 阚家义, 彭灿. 11种盐酸小檗碱片剂在不同溶出度介质中溶出度曲线特征的比较[J]. 中国药学(英文版), 2020, 29(2): 102-112.
[5]	樊文玲, 徐艳, 张心怡, 狄留庆, 李磊. 三元固体分散体提高利多卡因溶解度研究[J]. 中国药学(英文版), 2020, 29(1): 55-65.
[6]	刘蒸生, 郝海军, 范明松. 槲皮素磷脂复合物固体分散体和固体分散体的制备及评价[J]. 中国药学(英文版), 2019, 28(12): 868-877.
[7]	张玲玲, 张慧文, 武世奎, 刘宏, 李静媛, 董馨, 夏慧敏, 王焕芸. UPLC-Q-Exactive-MS 同时测定三臣丸中六种活性成分的药代动力学研究[J]. 中国药学(英文版), 2019, 28(11): 812-824.
[8]	杨绪朋, 仰浈臻, 张泸, 孙琪, 齐宪荣. 采用无表面活性剂体系合成不同形貌金纳米星[J]. 中国药学(英文版), 2019, 28(9): 641-649.
[9]	李展韬, 廖嫒, 刘曼, 张爽, 冯振汉, 王光雪, 王景茹, 徐美琦, 李卓越, 段晓川, 郝艳丽, 郑秀钗, 李惠, 纳沁, 张华, 刘碧林, 张烜. 聚氨基胺-聚乙二醇-聚氨基胺共聚物的合成及其含阿霉素凝胶的制备与评价[J]. 中国药学(英文版), 2019, 28(5): 316-328.
[10]	尹雅杰, 张小飞, 崔征, 曲伟, 何冰, 代文兵, 张华, 王学清, 张强. 热熔挤出法制备的非诺贝特纳米骨架系统的体外释放和口服生物利用度研究[J]. 中国药学(英文版), 2019, 28(5): 329-338.
[11]	李飘飘, 闫仪, 张海涛, 王茹, 韩壶壶, 王坚成. 载siRNA的壳聚糖外壳磷酸钙纳米粒治疗宫颈癌研究[J]. 中国药学(英文版), 2018, 27(8): 517-529.
[12]	邹洋, 靳尧, 周远航, 何楚瑜, 邓运强, 韩诗迪, 周楚杭, 李馨儒, 周艳霞, 刘艳. 双重pH敏感的聚合物-阿霉素偶联物胶束的制备与表征[J]. 中国药学(英文版), 2018, 27(8): 530-539.
[13]	邓运强, 靳尧, 何楚瑜, 邹洋, 周远航, 韩诗迪, 周楚航, 刘琦, 李馨儒, 周艳霞, 刘艳. 靶向小肠PepT1的碳酸钙纳米颗粒的制备与表征[J]. 中国药学(英文版), 2018, 27(6): 397-407.
[14]	张文茜, 彭光华, 宋茂远, 王佳星, 殷梦雅, 李佳佳, 刘雅婕, 张媛媛, 李馨儒. 克拉霉素脂质体的制备及体内外抗菌评价[J]. 中国药学(英文版), 2018, 27(6): 408-414.
[15]	屈小又, 邹洋, 靳尧, 周远航, 王子琪, 何楚瑜, 邓运强, 李馨儒, 周艳霞, 刘艳. 紫杉醇的聚(2-乙基-2-噁唑啉)-维生素E琥珀酸酯pH敏感聚合物胶束的制备与体外表征[J]. 中国药学(英文版), 2017, 26(8): 582-588.