A NOVEL NANOGEL FORMULATION OF FINASTERIDE FOR TOPICAL TREATMENT OF ANDROGENETIC ALOPECIA: DESIGN, CHARACTERIZATION AND IN VITRO EVALUATION
DOI:
https://doi.org/10.22159/ijap.2021v13i4.41599Keywords:
Nanoparticles (NP), Androgenetic alopecia, Nano lipid carrier (NLC), Finasteride (FSD)Abstract
Objective: The present paper describes the development and evaluation of a Novel Finasteride (FSD) nanogel topical delivery for the treatment of Androgenetic Alopecia. Nano-based topical formulation was chosen to enhance the solubility, permeability, biocompatibility of drug and to overcome the problems associated with the oral delivery of finasteride.
Methods: Various trails batches were prepared by using probe sonication method. Based on stability studies and particle size, NP4 trail was optimized which exhibited a spherical shape with a mean diameter of 113.80±0.72, the polydispersity of 0.28±0.01, zeta potential of-25.2 mV, drug entrapment efficiency of 92.67±0.47 %, and drug loading of 6.15±0.02 %. Storage stability studies demonstrated that the particle size and entrapment efficiency were not changed during 3 mo both at 4 °C and room temperature. Finasteride (FSD) NLCs were characterized for particle size by scanning electron microscope (SEM), chemical state by X-Ray diffraction (XRD), physical stability by centrifugation and thermodynamic stability by Freeze-thaw method. These prepared nanoparticles were transformed into topical nanogel and further evaluated.
Results: Among the different trails, C2 trail of NLC gel has shown excellent gelling capacity, clear appearance, good viscosity characteristics and was selected for further evaluation studies. Batches of topical nanogel were characterized through pH, homogeneity, spreadability, viscosity, drug content and in vitro drug release study. Based on pH (6.5-6.8), drug content (91.25±0.9%), spreadability (6.7 cm/sec), C2 batch was subjected to In vitro skin occlusivity study, in-vitro release study and In vitro heamolysis study.
Conclusion: The percent cumulative drug release for Finasteride (FSD) gel was found to be 758.52±1.49 µg at 24 h which is quite higher than plain gel and Finasteride (FSD) gel showed maximum occlusiveness and excellent spreadability and found to be stable. In conclusion, prepared Finasteride (FSD) Nanogel could be used with promising potential for the treatment of Androgenetic Alopecia.
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Salisbury BH, Tadi P. 5 Alpha reductase inhibitors. Treasure Island (FL): StatPearls Publishers; 2020.
Divya S, Shyam SR. A model for docking finasteride to 5α-reductase. Online J Bio Inform 2019;20:182-93.
Lee SW, Juhasz M, Mobasher P, Ekelem C, Mesinkovska NAA. Systematic review of topical finasteride in the treatment of androgenetic alopecia in men and women. J Drugs Dermatol 2018;17:457–63.
Roque LV, Dias IS, Cruz N, Rebelo A, Roberto A, Rijo P, et al. Design of finasteride-loaded nanoparticles for potential treatment of alopecia. Skin Pharmacol Physiol 2017;30:197-204.
Lademann J, Richter H, Teichmann A, Otberg N, Blume Peytavi U, Luengo J, et al. Nanoparticles-an efficient carrier for drug delivery into the hair follicles. Eur J Pharm Biopharm 2007;66:159-64.
Ahlin GP, Kristl J. The manufacturing techniques of drug-loaded polymeric nanoparticles from preformed polymers. J Microencapsulation 2011;28:323-35.
Couvreur P, Barratt G, Fattal E, Legrand P, Vauthier C. Nanocapsule technology: a review. Crit Rev Ther Drug Carrier Syst 2002;19:99-134.
Reis CP, Roque LV, Baptista M, Rijo P. Innovative formulation of nystatin particulate systems in toothpaste for candidiasis treatment. Pharm Dev Technol 2016;21:282-7.
Madheswaran T, Baskaran R, Thapa RK, Rhyu JY, Choi HY, Kim JO, et al. Design and in vitro evaluation of finasteride-loaded liquid crystalline nanoparticles for topical delivery. AAPS PharmSciTech 2013;14:45-52.
Franklin SJ, Younis US, Myrdal PB. Estimating the aqueous solubility of pharmaceutical hydrates. J Pharm Sci 2015;105:1914–9.
Sharma A, Baldi A. Nanostructured lipid carriers: a review. J Dev Drugs 2018;7:2.
Priyanka J, Parshotam M, Senshang L. Transdermal delivery of diclofenac using water-in-oil microemulsion: formulation and mechanistic approach of drug skin permeation. Pharm Dev Technol 2014;19:373-84.
Ranpise NS, Korabu SS, Ghodake VN. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride. Colloids Surf B 2014;116:81-7.
Chen CC, Tsai TH, Huang ZR, Fang JY. Effects of lipophilic emulsifiers on the oral administration of lovastatin from nanostructured lipid carriers: physicochemical characterization and pharmacokinetics. Eur J Pharm Biopharm 2010;74:474-82.
Ranpise NS, Korabu SS, Ghodake VN. Second-generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride. Colloids Surf B 2014;116:81-7.
Slavomira D, Joana A, Garcia ML, Erik R, Eliana BS. Formulating fluticasone propionate in novel PEG-containing nanostructured lipid carriers (PEG-NLC). Colloids Surf B 2010;75:538–42.
Nasr M, Mansour S, Mortada ND, El Shamy AA. Lipospheres as carriers for topical delivery of aceclofenac: preparation, characterization and in vivo evaluation. AAPS PharmSciTech 2008;9:154-62.
Patel D, Dasgupta S, Dey S, Roja Ramani Y, Ray S, Mazumder B. Nanostructured lipid carriers (NLC)-based gel for the topical delivery of aceclofenac: preparation, characterization, and in vivo evaluation. Sci Pharm 2012;80:749-64.
Bhaskar K, Anbu J, Ravichandiran V, Venkateswarlu V, Rao YM. Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies. Lipids Health Dis 2009;8:6.
Malgope A, Murthy P, Ramani R, Dey S. Development of nano-emulsion as carrier for transdermal delivery of valsartan. Int J Pharm Chem Sci 2013;2:1655-65.
Kotta S, Khan AW, Ansari S, Sharma R, Ali J. Formulation of nano-emulsion: a comparison between phase inversion composition method and high-pressure homogenization method. Drug Delivery 2015;22:455-66.
Meghana G, VVSNR K, Talluri S, Gunda R, Channareddy S, Ganesh G. 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.
Jannin V, Musakhanian J, Marchaud D. Approaches for the development of solid and semisolid lipid-based formulations. Adv Drug Delivery Rev 2008;60:734–46.
Inamdar Y, Rane B, Jain A. Preparation and Evaluation of beta sitosterol nanogel: a carrier design for targeted drug delivery system. Asian J Pharm Res Dev 2018;6:81-7.
Bhimashankar M, Sachin K, Kakasaheb RM. Formulation and evaluation of topical liposomal gel for fluconazole. Indian J Pharm Educ Res 2010;44:324-33.
Chen MX, Alexander KS, Baki G. Formulation and evaluation of antibacterial creams and gels containing metal ions for topical application. J Pharm (Cairo) 2016;5754349.
Maru AD, Lahoti SR. Formulation and evaluation of moisturizing cream containing sunflower wax. Int J Pharm Pharm Sci 2018;10:54-9.
Souto EB, Wissing SA, Barbosa CM, Muller RH. Development of controlled release formulation based on SLN and NLC for topical clotrimazole delivery. Int J Pharm 2004;278:71-7.
Jannin V, Musakhanian J, Marchaud D. Approaches for the development of solid and semisolid lipid-based formulations. Adv Drug Delivery Rev 2008;60:734–46.
Pund S, Pawar S, Gangurde S, Divate D. Transcutaneous delivery of leflunomide nanoemulgel: mechanistic investigation into physicomechanical characteristics, in vitro anti-psoriatic and anti-melanoma activity. Int J Pharm 2015;487:148-56.
Singh H, Gupta RD, Gautam G. Formulation development, characterization and in vitro-in vivo study of antihyperlipidemic drug rosuvastatin calcium-solid lipid nanoparticles. Asian J Pharm Clin Res 2018;11:436-43,
Khalil M, Ismail E, El-Baghdady K, Doaa M. Green synthesis of silver nanoparticles using olive leaf extract and its antibacterial activity. Arabian J Chem 2013;7:1131-9.
Patel D, Dasgupta S, Dey S, Roja Ramani Y, Ray S, Mazumder B. Nanostructured lipid carriers (NLC)-based gel for the topical delivery of aceclofenac: preparation, characterization, and in vivo evaluation. Sci Pharm 2012;80:749-64.
Pamudji JS, Mauludin R, Indriani N. Development of nanostructured lipid carrier formulation containing of retinyl palmitate. Int J Pharm Pharm Sci 2016;8:256-60.
Garcia Negrete CA, Jimenez de Haro MC, Blasco J, Soto M, Fernandez A. STEM-in-SEM high resolution imaging of gold nanoparticles and bivalve tissues in bioaccumulation experiments. Analyst 2015;140:3082-9.
Khurana S, Bedi PMS, Jain NK. Preparation and evaluation of solid lipid nanoparticles based nanogel for dermal delivery of meloxicam. Chem Phys Lipids 2013;175:65-72.
Rajinikanth PS, Chellian J. Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil. Int J Nanomed 2016;11:5067–77.
Pooja D, Panyaram S, Kulhari H, Rachamalla SS, Sistla R. Xanthan gum stabilized gold nanoparticles: characterization, biocompatibility, stability and cytotoxicity. Carbohydr Polym 2014;110:1-9.
Inayathulla, Goudanavar P, Ali M, Din Wani Su, Sreeharsha N. Formulation and evaluation of in-situ gel containing linezolid in the treatment of periodontitis. Int. J Appl Pharm 2021;13:79-86.
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