USE OF LACTIC ACID AND SPAN 80 IN THE FORMULATION OF LIPID BASED IMIQUIMOD VESICLES FOR GENITAL WARTS

Authors

  • Saroj Jain Department of Pharmaceutics, Hindu College of Pharmacy, Sonepat (Hr), India
  • Anupama Diwan Department of Pharmaceutical Sciences, Apeejay Stya University, Gurgaon (Hr), India
  • Satish Sardana Department of Pharmaceutics, Hindu College of Pharmacy, Sonepat (Hr), India

DOI:

https://doi.org/10.22159/ijpps.2017v9i2.15915

Keywords:

Ethosomes, Genital warts, Human papillomavirus, Imiquimod, Lipid based vesicles, Phospholipid

Abstract

Objective: The objective of present study was formulation development of imiquimod using lactic acid and span 80 for topical delivery to cure genital warts.

Methods: Lipid based vesicles (LBV) of 2% imiquimod were prepared with phospholipoin 90G, ethanol, lactic acid and span 80 using central composite design. The prepared vesicles were optimized statistically and characterized for particle size, zeta potential, percentage entrapment efficiency (% EE) and transmission electron microscopy (TEM). The optimized LBV were incorporated into gel formulation which was evaluated and compared with control gel and marketed formulation.

Results: The optimized vesicles had particle size 394.8±9.6 nm, zeta potential-16.5±2.5 mV, % EE 88.27±0.45 and TEM study confirmed the formation of vesicular structure with spherical shape. The gel formulation of imiquimod vesicles showed positive results like spreadability 14.3±0.34 gcm/s, viscosity 13500±1.67 cp, consistency 6.1±0.14 mm and extrudability 16.47±0.11 g/cm2. In vitro permeation amount of drug was remarkably lower (10.13 %) than control (87.17 %) and marketed formulation (27.46 %). Results of retained drug for both in vitro as well as in vivo permeation study and local accumulation efficiency (4.021±0.2292) were considerably higher for LBV gel than control (0.1008±0.002513) and marketed formulation (0.8314±0.0300). To understand the mechanism of interaction between skin and vesicles, fourier transform infra-red spectroscopy studies were also done. Results of skin irritancy test and histological examination revealed biocompatible nature of formulation.

Conclusion: Results of in vitro and in vivo studies indicated that this vesicle gel formulation provided efficient and site specific dermal delivery of imiquimod for cure of genital warts.

Downloads

Download data is not yet available.

References

Sexually transmitted diseases treatment guidelines. Centres for disease control and prevention. MMWR Recomm Rep 2002;51:1-78

Karnes JB, Usatine RP. Management of external genital warts. Am Fam Physician 2014;90:312-8.

Karthigeyan K. Cervical cancer in India and HPV vaccination. Indian J Med Paediatr Oncol 2012;33:7-12.

Cox JT, Petry KU, Rylander E, Roy M. Using imiquimod for genital warts in female patients. J Womens Health 2004;13:265-71.

Jubin Ryu F, Clarissa Yang A. Review of topical imiquimod in the management of basal cell carcinoma, actinic keratoses, and other skin lesions. Clin Med Ther 2009;1:1557–75.

Bhowmik D, Gopinath H, Kumar BP, Duraivel S, Kumar KPS. Recent advances in novel topical drug delivery system. Text Prax Int 2012;1:12-31.

Date AA, Naik B, Nagarsenker MS. Novel drug delivery systems: potential in improving topical delivery of antiacne agents. Skin Pharmacol Physiol 2006;19:2-16.

Fox CB, Sivananthan SJ, Duthie MS, Vergara J, Guderian JA, Moon E, et al. A nanoliposome delivery system to synergistically trigger TLR4 AND TLR7. J Nanobiotechnol 2014;12:1-18.

Touitou E. Composition of applying active substance to or through the skin. US Patent: 1996. p. 5, 540, 934.

Kaur LP, Guleri TK. Topical gel: a recent approach for novel drug delivery. Asian J Biomed Pharm Sci 2013;3:1-5.

Shinde M, Gharge V, Gurjar M, Shah M. Effect of penetration enhancer on the in vitro ex vivo permeation of diclofenac gel. Asian J Pharm Clin Res 2014;7:255-9.

Akiladevi D, Basak S. Ethosomes-a noninvasive approach for transdermal drug delivery. Int J Curr Pharm Res 2010;2:1-4.

Touitou E, Dayan N, Bergelson L, Godin B, Eliaz M. Ethosomes-novel vesicular carriers for enhanced delivery: characterization and skin penetration properties. J Controlled Release 2000;65:403-18.

Shen LN, Zhang YT, Wang Q, Xu L, Feng NP. Enhanced in vitro and in vivo skin deposition of apigenin delivered using ethosomes. Int J Pharm 2014;460:280-8.

Sheer A, Chauhan M. Ethosomes as vesicular carrier for enhanced transdermal delivery of ketoconazole-formulation and evaluation. J Pharm Cosmetol 2011;1:1-14.

Rao Y, Zheng F, Zhang X, Gao J, Liang W. In vitro percutaneous permeation and skin accumulation of finasteride using vesicular ethosomal carrier. AAPS PharmSciTech 2008;9:860-5.

Wavikar P, Vavia P. Nanolipidgel for enhanced skin deposition and improved antifungal activity. AAPS PharmSciTech 2013;14:222-33.

Pawar DP, Shamkuwar PB. Formulation and evaluation of herbal gel containing lantana camara leaves extract. Asian J Pharm Clin Res 2013;6:122-4.

Meghana G, Narayana Reddy Karri VVS, Talluri SV, Gunda R, Chennareddy SR, Ganesh GNK. Formulation and evaluation of tolnaftate loaded topical liposomal gel for effective skin drug delivery to treat fungal diseases. J Chem Pharm Res 2014;6:856-66.

Patel TN, Patel MM. Preparation and evaluation of imiquimod loaded solid lipid nanoparticles based topical gel formulation: part-1. J Biochem Pharmacol Res 2013;2:37-46.

Jain S, Tiwary AK, Sapra B, Jain NK. Formulation and evaluation of ethosomes for transdermal delivery of lamivudine. AAPS PharmSciTech 2007;8:111-9.

De PD, Martins CA, Entley M, Vitoria LB. Development and validation of HPLC method for imiquimod determination in skin penetration studies. Biomed Chromatogr 2008;22:1416-23.

Jain S, Diwan A, Sardana S. Development and validation of UV spectroscopy and RP-HPLC methods for estimation of imiquimod Int J Pharm Sci Rev Res 2015;35:16-21.

Ma M, Wang J, Fang G, Lei M, Tan F, Li N. Development of nanovesicular systems for dermal Imiquimod delivery: physicochemical characterization and in vitro/in vivo evaluation. J Mater Sci Maters Med 2015;26:192.

Gaur PK, Purohit S, Mishra S. Development of aceclofenac nanovesicular system using biomaterial for transdermal delivery: physical characterization, ex vivo, in vivo and anti-inflammatory studies. J Biomater Sci Polym Ed 2013;24:2126-41.

Panchaxari DM, Pampana S, Pal T, Devabh Maheshwari RGS, Tekade RK, Sharma PA, et al. Ethosomes and ultradeformable liposomes for transdermal delivery of clotrimazole: a comparative assessment. Saudi Pharm J 2012;20:161–70.

Aktuni B, Aravapalli AK. Design and characterization of diclofenac diethylamine transdermal patch using silicon and acrylic adhesives combination. DARU 2013;21:1-14.

Gupta V, Dhote V, Paul VN, Trivedi P. Development of novel topical drug delivery system containing cisplatin and imiquimod for dual therapy in cutaneous epithelial malignancy. J Liposome Res 2014;24:50–162.

Dubey V, Mishra D, Nahar M, Jain V, Jain NK. Enhanced transdermal delivery of an anti-HIV agent via ethanolic liposomes. Nanomed: Nanotechnol Biol Med 2010;6:590–6.

Elsayed MA, Abdallah YO, Naggar FV, Khalafallah NM. Lipid vesicles for skin delivery of drugs: reviewing three decades of research. Int J Pharm 2006;332:1–16.

Zhang JP, Wei YH, Zhou Y, Li YQ, Wu XA. Ethosomes, binary ethosomes and transfersomes of terbinafine hydrochloride: a comparative study. Arch Pharm Res 2012;35:109–17.

Guo F, Wang JP, Ma M, Tan FP, Li N. Skin targeted lipid vesicles as novel nano-carrier of ketoconazole: characterization, in vitro and in vivo evaluation. J Mater Sci 2015;26:175.

Rawat AS, Kumar MS, Khurana B, Mahadevan N. Proniosome gel. Int J Res Ayurveda Pharm 2013;3:3-10.

Akhtar N, Pathak K. Cavamax W7 composite ethosomal gel of clotrimazole for improved topical delivery: development and comparison with ethosomal gel. AAPS PharmSciTech 2011;13:344-55.

Guiling L, Yating F, Chao F, Xinru L, Xiaoning W, Mei L, et al. Tacrolimus-loaded ethosomes: physicochemical characterization and in vivo evaluation. Eur J Pharm Biopharm 2012;82:49–57.

Shiny A, Toomu MC, Dhurke RK. Enhanced dermal delivery of nadifloxacin using liposomes. Int J Appl Pharm 2016;8:53-9.

Published

01-02-2017

How to Cite

Jain, S., A. Diwan, and S. Sardana. “USE OF LACTIC ACID AND SPAN 80 IN THE FORMULATION OF LIPID BASED IMIQUIMOD VESICLES FOR GENITAL WARTS”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 9, no. 2, Feb. 2017, pp. 292-01, doi:10.22159/ijpps.2017v9i2.15915.

Issue

Section

Original Article(s)