CELASTROL NANOEMULGEL FORMULATION AND IN VITRO PENETRATION TEST
DOI:
https://doi.org/10.22159/ijpps.2020v12i8.37167Keywords:
Celastrol (Cst), Transdermal nanoemulgel, Anti-inflammatory, Franz diffusion cells (SDF)Abstract
Objective: To obtain formulations of Celastrol (Cst) nanoemulgel via transdermal route. Celastrol is classified in BCS 4 class as an anti-inflammatory drug. These routes are considered to reduce the risk of Celastrol side effects and have the same characteristics as skin morphology.
Methods: Celastrol nanoemulgel was prepared by a high-pressure homogenizer (HPH) technique. To find the optimum nanoemulsion area by using the Chemix 7.00 ternary phase program. Celastrol nanoemulgel was evaluated by measuring the particle size, PDI, morphology, zeta potential, stability tests and in vitro using Franz diffusion cell
Results: Results showed the ideal formula based on the ternary phase diagram using chemix 7.00 is oil: smix: water (5:45:50), with particle size 89.9±5 nm, PDI 0.1, and zeta-21 mV. The morphological shape is quite spherical ≤ 100±5 nm. The pH value of this formula is 4.5, which compatible with the pH of the skin. The highest recovery rate of Celastrol and encapsulation efficiency (EE) were formulas 3 μg/ml and 5 μg/ml, with EE 91.70% and 94.54%, respectively. In vitro test results showed that the formula 3 μg/ml and 5 μg/ml give better penetration results than the formula 2.5 μg/ml. Thus, Celastrol nanoemulgel formula has good potential to be developed as a transdermal anti-inflammatory drug.
Conclusion: Transdermal nanoemulgel containing Celastrol has been successfully developed with particle size ≤ 200±2 nm.
Downloads
References
Xinqiang S, Yu Z, Erqin D, Hongtao D, Lei W. International immunopharmacology mechanism of action of celastrol against rheumatoid; 2019. DOI:10.1016/j.intimp.2019.105725
Joshi V, Venkatesha SH, Ramakrishnan C, Nanjaraj Urs AN, Hiremath V, Moudgil KD, et al. Celastrol modulates inflammation through inhibition of the catalytic activity of mediators of the arachidonic acid pathway: secretory phospholipase A 2 group IIA, 5-lipoxygenase and cyclooxygenase-2. Pharmacol Res IJSI 2016;2:204-17.
Gunasekaran T, Haile T, Nigusse T, Dhanaraju MD. Nanotechnology: an effective tool for enhancing bioavailability and bioactivity of phytomedicine. Der Pharm Lett 2014;2 Suppl 6:84-98.
Peng X, Wang J, Song H, Cui D, Li L, Li J, Liu Y. Optimized preparation of celastrol-loaded polymeric nanomicelles using rotatable central composite design and response surface methodology. J Biomed Nanotechnol Int J Drug Delivery 2012;3:83–94.
Meng S, Sun L, Wang L, Lin Z, Liu Z, Xi L, Wang Z. Colloids and surfaces B: Biointerfaces loading of water-insoluble celastrol into niosome hydrogels for improved topical permeation and anti-psoriasis activity. Colloids Surf B 2019;15:373–9.
Kang Q, Liu J, Zhao Y, Liu X, Liu X, Wang Y. Transdermal delivery system of nanostructured lipid carriers loaded with celastrol and indomethacin: optimization, characterization and efficacy evaluation for rheumatoid arthritis. Artif Cells Nanomed Biotechnol 2018;46 Suppl 3:585–97.
Song J, Shi F, Zhang Z, Zhu F, Xue J, Tan X. Jia X. Formulation and evaluation of celastrol-loaded liposomes. Molecules 2011;16:7880–92.
Freag MS, Saleh WM, Abdallah OY. Self-assembled phospholipid-based phytosomal nanocarriers as promising platform for improving oral bioavailability of the anticancer celastrol. Int J Pharm 2018;535:18-26.
Gupta A, Eral HB, Hatton TA, Doyle PS. Nanoemulsions: formation, properties and applications. Increasing in vitro penetration. Asian J Pharm Clin Res 2017;10:294-8.
Alvarado HL, Abrego G, Souto EB, Garduño Ramirez ML, Clares B, Garcia ML, et al. Nanoemulsions for dermal controlled release of oleanolic and ursolic acids: in vitro, ex vivo and in vivo characterization. Colloids Surf B 2015;130:40–7.
Shaker DS, Ishak RAH, Ghoneim A, Elhuoni MA. Nanoemulsion: a review on mechanisms for the transdermal delivery of hydrophobic and hydrophilic drugs. MDPI; 2019.
Dubois V, Breton S, Linder M, Fanni J, Parmentier M. Fatty acid profiles of 80 vegetable oils with regard to their nutritional potential. Eur J Lipid Sci Technol 2007;109:710–32.
Rai VK, Mishra N, Yadav KS, Yadav NP. Nanoemulsion as pharmaceutical carrier for dermal and transdermal drug delivery: formulation development, stability issues, basic considerations and applications. Controlled Release 2018;270:203–25.
Syed HK, Peh KK. Identification of phases of various oil, surfactant/co-surfactants and water system by ternary phase diagram. APP Drug Res 2014;71:301–9.
Yadav SA, Singh D, Poddar S. Nanoemulsion system for transdermal drug delivery of nimodipine. AJPC Res 2012;5:1–6.
Ernoviya E, Masfria M, Sinaga KR. Optimization and evaluation of topical ketoconazole nanoemulsion. AJPC Res 2018;11:5–8.
Galvao KCS, Vicente AA, Sobral PJA. Development, characterization, and stability of O/W pepper nanoemulsions produced by high-pressure homogenization. Food Bioproc Tech 2018;11:355–67.
Seppic. Sepigel TM 305; 2018.
Ari Susanti. Penetration of pyroxicam in the solid dispersion system across the lipid membrane of the sepigel form. Surabaya Indonesia; 2005.
Morsy MA, Abdel latif RG, Nair AB, Shehata TM. Preparation and evaluation of atorvastatin-loaded nanoemulgel on wound-healing efficacy. Pharmaceutics 2019;11:1–15.
Qi J, Lu Y, Wu W. Absorption, disposition and pharmacokinetics of solid lipid nanoparticles. Curr Drug Metab 2012;13:418–28.
Ugur B, Cetin M, Orgul D, Taghizadehghalehjoughi A, Hac A, Hekimoglu S. Formulation and in vitro evaluation of topical nanoemulsion and nanoemulsion-based gels containing daidzein. J Drug Delivery Sci Technol 2019;52:189–203.
Martin A. Book review: physical pharmacy: physical chemical rinciples in the pharmaceutical sciences. 3rd Ed. Drug Intelligence and Clinical Pharmacy; 2016.
Maha HL, Sinaga KR. Formulation and evaluation of miconazole nitrate nanoemulsion and cream. AJPC Res 2018;3:3–5.
Mishra. Improvement of drug penetration through the skin by using nanostructured lipid carriers (NLC). IJPPR 2016;6:1–16.
Peng X, Wang J, Song H, Cui D, Li L, Li J, et al. Optimized preparation of celastrol-loaded polymeric nanomicelles using rotatable central composite design and response surface methodology. J Biomed Nanotech 2012;8:491–9.
Gururaj. Localized in situ nanoemulgel drug delivery system of quercetin for periodontitis: MDPI; 2018.
Alam MS, Ali MS, Alam N, Alam MI, Anwer T, Imam F, et al. Design and characterization of topical nanostructure gel of betamethasone dipropionate for psoriasis. J Appl Pharm Sci 2012;2:148–58.
Mardikasari SA, Jufri M, Djajadisastra J. Formulation and in vitro penetration study of topical dosage form of nanoemulsion from genistein of sophora japonica Linn. J Ilmu Kefarmasian Indonesia 2016;14:190–8.
Singh BP, Kumar B, Jain SK, Shafaat K. Development and characterization of a nanoemulsion gel formulation for transdermal delivery of carvedilol. Int J Drug Dev Res 2012;4:151–61.
Onyeabor F, Paik A, Kovvasu S, Ding B, Lin J, Wahid A, et al. Optimization of preparation and preclinical harmacokinetics of celastrol-encapsulated silk fibroin nanoparticles in the rat. Molecules 2019;24:3271.
Gu Y, Tang X, Yang M, Yang D, Liu J. Transdermal drug delivery of triptolide-loaded nanostructured lipid carriers: preparation, pharmacokinetic, and evaluation for rheumatoid arthritis. Int J Pharm 2019;554:235–44.
Shafaat K, Kumar B, Das SK, Ul Hasan R, Prajapati SK. Novel nanoemulsion as vehicles for transdermal delivery of clozapine: in vitro and in vivo studies. Int J Pharm Sci 2013;5 (Suppl 3):126–34.
Abulfadhel JN Al-Shaibani, Karrar MH Al-Gburi, Karrar TKA. Original article design and characterization of candesartan cilexetil oral nanoemulsion containing garlic oil. Int J Appl Pharm 2019;11:116-24.
Danaei M, Dehghankhold M, Ataei S, Davarani FH, Javanmard R, Dokhani A, et al. Impact of particle size and polydispersity index on the clinical applications of lipidic nanocarrier systems. Pharmaceutics 2018;10:57.
Akbas E, Soyler B, Oztop MH. Formation of capsaicin loaded nanoemulsions with high-pressure homogenization and ultrasonication. LWT 2018;96:266–73.
Hanifah M, Jufri M. Formulation and stability testing of nanoemulsion lotion containing centella asiatica extract. JYP 2018;1:2-7.
Yukuyama MN, Kato ETM, de Araujo GLB, Lobenberg R, Monteiro LM, Lourenço FR, et al. Olive oil nanoemulsion preparation using high-pressure homogenization and D-phase emulsification–a design space approach. J Drug Delivery Sci Technol 2019;49:622–31.
Zha J, Zhang Q, Li, M, Wang JR, Mei X. Improving dissolution properties by polymers and surfactants: a case study of celastrol. J Pharm Sci 2018;107:2860–8.
Amin N, Das B. A review on formulation and characterization of nanoemulsion. Int J Curr Pharm Res 2019;11:1-5.
Published
How to Cite
Issue
Section
