OPTIMIZATION AND IN VITRO EVALUATION OF THE RELEASE OF CLASS II DRUG FROM ITS NANOCUBOSOMAL DISPERSION
Keywords:Cubosomes, Erythromycin, GMO, Poloxamer 407, Nanotechnology
Objective: This work involves investigation and evaluation of the factors that affect the preparation and the release of the model class II drug (erythromycin) to optimize the efficiency of its prepared nanocubosomal dispersion to give very fast initial burst effect within the first hour that can continue for further two hours.
Methods: The work involved preparation of ten formulas of cubosomal dispersion by emulsifying different concentrations of glyceryl monooleate (GMO) (lipid content)/surfactant mixtures which were nano-sized and characterized morphologically by Transmission electronic microscopic (TEM), zeta potential, particle size, polydispersity index (pdI), pH, entrapment efficiency, conductivity test, dilution test and in vitro drug release.
Results: The selected nanocubosomal formula (F1) showed pH (7.41), particle size (315.05 nm), pdI (0.194), zeta potential (-30.852), entrapment efficiency (91%) and gave a 70% drug release within the first hour of the in vitro test and continued until it gave 96.3% drug release with further 2 h.
Conclusion: this work succeeded in preparing optimized cubosomal dispersion for erythromycin using different GMO/poloxamer 407 percent. The optimum formula gave an immediate release of the model drug (erythromycin) and it was ready to be incorporated in any suitable dosage form to give fast onset of action.
Date A, Naik B, Nagarsenker MS. Novel drug delivery systems: potential in improving topical delivery of antiacne agents. Skin Pharma Physio 2005;19:2-16.
Sherif S, Bendas ER, Badawy S. The clinical efficacy of cosmeceutical application of liquid crystalline nanostructured dispersions of alpha lipoic acid as anti-wrinkle. Eur J Pharm Biopharm 2014;86:251-9.
Anbarasan B, Fatima GX, Shanmuganathan S. An overview of cubosomes-smart drug delivery system. Sri Rama J Med 2015;8:1-4.
He H. Cubosomes from hierarchical self-assembly of poly (ionic liquid) block copolymers. Nat Commun 2017;8:1-8.
Gaynor M, Mankin AS. Macrolide antibiotics: binding site, mechanism of action, resistance. Curr Top Med Chem 2003;3:949-61.
Morsi NM, Abdelbary GA, Ahmed MA. Silver sulfadiazine based cubosome hydrogels for the topical treatment of burns: development and in vitro/in vivo characterization. Eur J Pharma BioPharma 2014;86:178-89.
Sana K, Poorva J, Sourabh J, Richa Jain, Saurabh B, Aakanchha J. Topical delivery of erythromycin through cubosomes for acne. Pharma Nanotech 2018;6:38-47.
Ghosh V, Mukherjee A, Chandrasekaran N. Ultrasonic emulsification of food-grade nanoemulsion formulation and evaluation of its bactericidal activity. Ultrasonics Sonochem 2013;20:338-44.
Shweta K, Ganesh K, Preeti K. Development and in vitro characterization of the ocular insert containing erythromycin. Int Res J Pharma 2012;3:246-50.
Nasra M, Ghoraba MK, Abdelazem A. In vitro and in vivo evaluation of cubosomes containing 5-fluorouracil for liver targeting. Acta Pharma Sinica 2015;5:79-88.
McClements D. Colloidal basis of emulsion color. Curr Opin Colloid Interface Sci 2002;7:451-5.
Beg S, Jenaa SS, Patraa CN, Rizwanb M, Swaina S, Sruti J, et al. Development of solid self-nano emulsifying granules (SSNEGs) of ondansetron hydrochloride with enhanced bioavailability of potential colloids and surfaces. Biointerfaces 2013;101:414-23.
Setya S, Negi P, Razdan D, Talegaonkar DS. Design, development and in vitro investigation of water in oil nanoemulsion for transdermal delivery. World J Pharma Pharmaceutical Sci 2014;3:1495-512.
Ravi PR, Aditya N, Patil S, Cherian L. Nasal in-situ gels for delivery of rasagiline mesylate: improvement in bioavailability and brain localization. Informa Healthcare 2015;22:903-99.
Skoog DA, West DM, Holler FJ, Stanley RC. Fundamentals of analytical chemistry. 9th edition. Thomson-Brooks/Cole, USA; 2014;9:658-64.
Bachhav JK, Bhairav BA, Saudagar RB. Formulation and evaluation of topical emulgel of ketoconazole by cubosomal technique. World J Pharma Res 2017;6:567-88.
Danaei M, Dehghankhold M, Ataei S, Hasanzadeh F, Javanmard R, Dokhani A, et al. Impact of particle size and polydispersity index on the clinical applications of lipidic nanocarrier systems. Pharmaceutics 2018;10:1-17.
Daware SU, Saudagar RB. Formulation and development of cubosomes loaded emulgel of fluconazole. Eur J Bio Med Pharma Sci 2017;4:321-31.
Rainer H. Zeta potential and particle loading in laboratory practice: an introduction to theory, practical measurement performance, data interpretation. 24th ed. scientific publishing company; 1996.
Hoeller S, Sperge A, Valenta C. Lecithin based nanoemulsions: a comparative study of the influence of non-ionic surfactants and the cationic phytosphingosine on physicochemical behavior and skin permeation. Int J Pharm 2009;370:181-6.
Tadros TF. Emulsion formation and stability. 1st ed. Germany: Wiley-VCH Verlag Gmb H and Co. KGaA; 2013.
Chhabra G, Chuttani K, Mishra AK, Pathak K. Design and development of nanoemulsion drug delivery system of amlodipine besilate for improvement of oral bioavailability. Drug Dev Pharm 2011;37:907-16.
USP 32. NF27UP. USA, Rockville MD: The United State pharmacopeial convention Inc; 2008.
Harivardhan LR, Murthy RS. Etoposide-loaded nanoparticles made from glyceride lipids: formulation, characterization, in vitro drug release, and stability evaluation. AAPS Pharma Sci Tech 2005;6:158-66.
Kalra R. Development and characterization of nanoemulsion formulations for transdermal delivery of aceclofenac. Int J Drug Form Res 2010;1:359-86.
Almajidi YQ, Zainab HM, Maraie NK. Preparation and in vitro evaluation of montelukast sodium oral nanoemulsion. Int J Appl Pharm 2018;10:49-53.
Salwa S, Azza A, Amany OK. Etodolac transdermal cubosomes for the treatment of rheumatoid arthritis: ex vivo permeation and in vivo pharmacokinetic studies. Drug Delivery 2017;24:846-56.
Maraie NK, Almajidi YQ. Effect of different mucoadhesive polymers on the release of ondansetron HCl from intranasal mucoadhesive in situ gel. Afr J Plant Sci 2017;17:76-84.
Wesam RK, Shohei S, Ichiro H, Hiroaki T, Kenji S. A novel chemical enhancer approach for transdermal drug delivery with C17 monoglycerol ester liquid crystal forming lipid. J Oleo Sci 2017;66:443-54.
Thakkar V, Korat V, Baldaniya L, Gohel M, Gandhi T, Patel N. Development and characterization of the novel hydrogel containing an antimicrobial drug for treatment of burns. Int J Pharma Invest 2018;6:158-68.
Riccia EJ, Lunardi LO, Nanclares DMA, Marchetti JM. Sustained release of lidocaine from poloxamer 407 gels. Int J Pharm 2005;288:235-44.
Shimadzu corporation analytical Instruments Division. Shimadzu reference manual. Kyoto, Japan; 2001.