ABSTRACT:
The present work is aimed to design, develop and characterize a novel nanostructured lipid carrier system based formulation for selective and customized delivery of adapalene and Vit-E for effective management of acne vulgaris. Adapalene loaded nanostructured lipid carriers were developed by modified melt dispersion ultrasonication technique, followed by cooling and high speed mechanical stirring. Principally in the process glyceryl tristearin was used as solid lipid and oleic acid as liquid lipid, phospholipid 90G was used as surfactant and carbopol was used as gelling material. The prepared nanocarriers were characterized in terms of particle size, zeta potential, polydispersity index, entrapment efficiency, transmission electron microscopy (TEM) and in-vitro drug release study. The particle size of optimized carrier was reported as 219.8nm. TEM analysis was also performed to assure particle size and shape of carrier system. Entrapment efficiency of optimized formulation was above 87.4%. The drug release from carrier have shown dual biphasic release pattern firstly the drug release rate was rapid which showed initial burst release pattern and subsequently sustained release pattern was observed which is required in treatment of acne. Then prepared and optimized formulation was subjected to skin permeation study in male Wistar rats. Formulation was also characterized for skin distribution study, skin irritation study and stability study of gel. So it was concluded in our research that this novel carrier system having adapalene and Vit-E can be a very innovative alternate of conventional antiacne therapy. In our research, drug is localized in superficial skin layer and systemic penetration of drug was avoided. Further, concrete research can open new avenues in antiacne treatment.
Cite this article:
Amit Kumar Jain, Parul Mehta. Co-administration of Adapalene loaded Nanostructured lipid carriers and Vitamin-E for management of acne. Research Journal of Pharmacy and Technology. 2023; 16(11):5067-3. doi: 10.52711/0974-360X.2023.00821
Cite(Electronic):
Amit Kumar Jain, Parul Mehta. Co-administration of Adapalene loaded Nanostructured lipid carriers and Vitamin-E for management of acne. Research Journal of Pharmacy and Technology. 2023; 16(11):5067-3. doi: 10.52711/0974-360X.2023.00821 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2023-16-11-15
REFERENCES:
1. Degitz K. Placzek M. Borelli C. Plewig G. Pathophysiology of acne. Journal of German Socienty of Dermatology. 2007; 5(4): 316–323. https://doi.org/10.1111/j.1610-0387.2007.06274.x
2. Irby C E. Yentzer B A. and Feldman S R. (2008). A review of adapalene in the treatment of acne vulgaris. The Journal of Adolescent Health : Official Publication of the Society for Adolescent Medicine. 2008; 43(5): 421-424. https://doi.org/10.1016/j.jadohealth.2008.06.005
3. Baghel S. Gidwani B. Kaur CD. Novel Drug Delivery Systems of Herbal Constituents Used in Acne. Asian Journal of Research in Pharmaceutical Sciences, 2017; 7(2): 57–67. https://doi.org/10.5958/2231-5659.2017.00009.1
4. Gharsan M AL. Sreeharsha N. Therapeutics of microneedling for skin repair. Asian Journal of Research in Pharmaceutical Sciences. 2022; 12(3): 199–204. https://doi.org/ 10.52711/2231-5659.2022.00035
5. Nasorallahi SA. Koohestani F. Naeimifar A. Samadi A. Vatanara A. et al Preparation and evaluation of adapalene nanostructured lipid carriers for targeted drug delivery in acne. Dermatologic Therapy, 2021; 34(2): 1–10. https://doi.org/10.1111/dth.14777
6. Umalkar D. Saudagar RB. Patel D.Rajesh K S. (2014). Formulation and Evaluation of Transferosomal gel of Isotretinoin for severe Acne. Research Journal of Topical and Cosmetic Sciences. 2014; 5(2): 39–45.
7. Bernard B A. Adapalene, a new chemical entity with retinoid activity. Skin Pharmacology : The Official Journal of the Skin Pharmacology Society, 1993; 6(1): 61–69. https://doi.org/10.1159/000211165
8. Aktürk AS. Güzel S. Bulca S. Demirsoy EO. Bayramgürler D. Bilen N. and Kıran, R. Effects of isotretinoin on serum vitamin E levels in patients with acne. International Journal of Dermatology, 2013; 52(3): 363–366. https://doi.org/10.1111/j.1365-4632.2012.05676.
9. Azulay M M. Bagatin, E. (2009). Cosmeceuticals vitamins. Clinics in Dermatology. 2009; 27(5): 469–474. https://doi.org/10.1016/j.clindermatol.2009.05.010
10. Keen M A. Hassan I. Vitamin E in dermatology. Indian Dermatology Online Journal. 2016; 7(4): https://journals.lww.com/idoj/Fulltext/2016/07040/Vitamin_E_in_dermatology.18.aspx
11. Pappas A. Liakou A. Zouboulis C C. Nutrition and skin. Reviews in Endocrine and Metabolic Disorders. 2016; 17(3): 443–448. https://doi.org/10.1007/s11154-016-9374-z
12. Jain AK. Jain A. Garg N K. Agarwal A., Jain, A. Jain S A Tyagi R K. Jain, R K. Agrawal H. Agrawal GP. et al Adapalene loaded solid lipid nanoparticles gel: an effective approach for acne treatment. Colloids and Surfaces. B, Biointerfaces. 2014; 121: 222–229. https://doi.org/10.1016/j.colsurfb.2014.05.041
13. Erawati T. Hariyadi D M. Rosita. N.Purwanti T. Comparison of the Release rate, Penetration and Physical stability of p-Methoxycinamic acid (PMCA) in Nanostructured Lipid Carriers (NLC), Solid Lipid Nanoparticle (SLN) and Nanoemulsion (NE) systems Research Journal of Pharmacy and Technology. 2021; 14(11): 5719–5724. https://doi.org/10.52711/0974-360X.2021.00994
14. Das S. Chaudhury A. Recent advances in lipid nanoparticle formulations with solid matrix for oral drug delivery. AAPS PharmSciTech. 2011; 12(1): 62–76. https://doi.org/10.1208/s12249-010-9563-0
15. Dsouza J I. More H N. Topical Anti-Inflammatory Gels of Fluocinolone Acetonide Entrapped in Eudragit Based Microsponge Delivery System. Research Journal of Pharmacy and Technology. 2008; 1(4): 502–506.
16. Madhumitha V. Sangeetha S. Transfersomes: A Novel Vesicular Drug Delivery System for Enhanced Permeation through Skin. Research Journal of Pharmacy and Technology 2020; 13(5): 2493–2501. https://doi.org/10.5958/0974-360X.2020.00445.X
17. Khurana S. Bedi P MS. Jain NK. Development of Nanostructured Lipid Carriers (NLC) for controlled delivery of mefenamic acid. Int Jouranl of Biomedical Nanoscience and Nanotechnology. 2012; 2(3-4): 232–250. https://doi.org/10.1504/IJBNN.2012.051218
18. Joshi M. Patravale V. Formulation and evaluation of nanostructured lipid carrier (NLC)-based Gel of Valdecoxib. Drug Development and Industrial Pharmacy 2006; 32: 911–918. https://doi.org/ 10.1080/03639040600814676.
19. Zhao X. Yang C. Yang K. Li K. Hu H. Chen D. Preparation and characterization of nanostructured lipid carriers loaded traditional Chinese medicine, zedoary turmeric oil. Drug Development and Industrial Pharmacy 2010; 36 (7): 773–780. https://doi.org/ 10.3109/03639040903485716
20. Ridolfi D M. Marcato P D. Justo G. Z. Cordi L. Machado D. Durán N. Chitosan-solid lipid nanoparticles as carriers for topical delivery of tretinoin. Colloids and Surfaces B: Biointerfaces. 2012; 9: 36–40. https://doi.org/10.1016/j.colsurfb.2011.11.051
21. Martins L A. Meneghini LZ. Junqueira C A. Ceni D C. Bergold A M. A Simple HPLC-DAD Method for Determination of Adapalene in Topical Gel Formulation. Journal of Chromatographic Science. 2011; 49(10): 796–800. https://doi.org/ 10.1093/chrsci/49.10.796
22. Ramezanli T. Bozena B. Kohn M. Development and Characterization of a Topical Gel Formulation of Adapalene-TyroSpheres and Assessment of Its Clinical Efficacy. Molecular Pharmaceutics 2018; 15(9): 3813–3822.https://doi.org/10.1021/acs.molpharmaceut.8b00318
23. Kumara G. Patrudub T B. Raoa MV B. Raoa T N. A Novel Method Development and Validation for Related Substances of Adapalene in Bulk Drug Product by HPLC. Research Journal of Pharmacy and Technology 2016; 9(12): 2234–2240. https://doi.org/10.5958/0974-360X.2016.00451.0
24. Fang JY. Fang CL. Liu CH. Su YH. Lipid nanoparticles as vehicles for topical psoralen delivery: solid lipid nanoparticles (SLN) versus nanostructured lipid carriers (NLC). European Journal of Pharmaceutics and Biopharmaceutics. 2008; 70(2): 633–640. https://doi.org/10.1016/j.ejpb.2008.05.008
25. Czernielewski J.Michel S. Bouclier M. Baker M. and Hensby, C. (2001). Adapalene biochemistry and the evolution of a new topical retinoid for treatment of acne. Journal of the European Academy of Dermatology and Venereology. 2001; 15(SUPPL. 3): 5–12. https://doi.org/10.1046/j.0926-9959.2001.00006.x
26. Danaei M. Dehghankhold M. Ataei S. Hasanzadeh Davarani F. Javanmard R.et al Impact of Particle Size and Polydispersity Index on the Clinical Applications of Lipidic Nanocarrier Systems. Pharmaceutics. 2018; 10(2): https://doi.org/10.3390/pharmaceutics10020057
27. Obeidat W M. Schwabe K. Müller R H. Keck C M. Preservation of nanostructured lipid carriers (NLC). European Journal of Pharmaceutics and Biopharmaceutics. 2010; 76(1): 56–67. https://doi.org/https://doi.org/10.1016/j.ejpb.2010.05.001
28. Kumar R. Singh B. Bakshi G. Katare O P. Development of liposomal systems of finasteride for topical applications: design, characterization, and in vitro evaluation. Pharmaceutical Development and Technology. 2007; 12(6): 591–601. https://doi.org/10.1080/10837450701481181