Development and Characterization of Mucinated Chitosan Microcomposite for Oral Insulin Delivery doi.org/10.26538/tjnpr/v4i11.27
Main Article Content
Abstract
The development of oral insulin is a vital tool in improving compliance in diabetic patients. The study aimed to develop oral insulin microparticles using mucin grafted chitosan as the carrier matrix and to study the in vitro and in vivo properties of the formulations. Insulin-loaded microparticles (IMP) were prepared by water-in-oil-in-water (w/o/w) double emulsion technique. Varying ratios of mucin to chitosan; 1:1 (FA1), 1:2 (FA2), 1:3 (FA3), and 1:4 (FA4) were used in the preparation of the microparticles. The loaded-microparticles were characterized in vitro by encapsulation efficiency (EE), particle size, morphology, and release studies. The in vivo hypoglycaemic effects of the IMP were studied in alloxan-induced diabetic rats. The results showed a recovery value of ≥ 73%, particles sizes ranging from 121.0 ± 0.04 µm to 142.6 ± 0.05 µm. EE% ranged from 91.1% to 93.7%. The in vitro release of insulin from the microparticles at 8 h were 30.5, 37.8, 49.0, and 58.2% for FA1-FA4, respectively. The in vivo hypoglycemic studies showed that orally administered IMPs significantly (p < 0.05) lowered the blood glucose and showed glucose reduction from 89.23 ± 1.72% at 0.5 h to 26.46 ± 4.02% in 12 h. Liver function tests showed no significant changes compared with the control. The results suggest that mucin grafted chitosan microparticles possess good potentials for oral delivery of insulin and offered sustained drug release effects which could be useful in the oral delivery of insulin.
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References
Abdallah M, Yuichi T, Hirofumi T. Design and evaluation of novel pH-sensitive chitosan nanoparticles for oral insulin delivery. Eur J Pharm Sci. 2011; 42: 445-451.
Kim IY, Seo SJ, Moon HS, Cho CS. Chitosan and its derivatives for tissue engineering applications. Biotechnol Adv. 2008; 26:1-21.
George M and Abraham TE. Polyionic hydrocolloids for the intestinal delivery of protein drugs: alginate and chitosan — a review. J Cont Rel. 2006; 114:1-14.
Makhlofa A, Tozukaa Y, Takeuchia H. Design and evaluation of novel pH-sensitive chitosan nanoparticles for oral insulin delivery. Eur J Pharm Sci. 2011; 42:445–451.
Wang J, Xu M, Cheng X, Kong M, Liu Y, Feng C, Chen X. Positive/negative surface charge of chitosan-based nanogels and its potential influence on oral insulin delivery. Carbohydr Polym. 2016; 136:867–874.
Li L, Jiang G, Yu W, Liu D, Chen H, Liu K, Zaizai T, Ziangdong K, Juming Y. Preparation of chitosan-based multifunctional nanocarriers overcoming multiple barriers for oral delivery of insulin. Mat Sci Eng. 2017; 70:278–286.
Adikwu MU. Mucins and their potentials. Trop J Pharm Res. 2006; 5(2):581-582.
Momoh MA, Emmanuel OC, Onyeto AC, Darlington Y, Kenechukwu FC, Ofokansi KC, Attama AA. Preparation of snail cyst and PEG-4000 composite carriers via PEGylation for oral delivery of insulin: An in vitro and in vivo evaluation. Trop J Pharm Res. 2019; 18:919–926.
Babiker A and Datta V. Lipoatrophy with insulin analogues in type I diabetes. Arch Dis Childhood. 2011; 96:101–102.
Ramineni SK, Cunningham LL, Dziubla TD, Puleo DA. Competing properties of mucoadhesive films designed for localized delivery of imiquimod. Biomaterials Sci. 2013; 1:753–762.
Lei Li, Liaoqing Y, Manman L, Liefeng Z. A cellpenetrating peptide mediated chitosan nanocarriers for improving intestinal insulin delivery. Carbohydr Polym. 2017; 174:182–189.
Pereira de SI, Moser T, Steiner C, Fichtl B, BernkopSchnurch A. Insulin loaded mucus permeating nanoparticles: Addressing the surface characteristics as feature to improve mucus permeation. Int J Pharm. 2016; 500(1-2):236– 244.
Roger E, Lagarce F, Garcion E, Benoit JP. Biopharmaceutical parameters to consider in order to alter the fate of nanocarriers after oral delivery. Nanomed (Lond). 2011; 5:287-306.
Arhewoh MI, Eraga SO, Maroh O. Transdermal delivery of bovine serum Albumin using snail mucin. East Cent Afr J Pharm Sci. 2014; 17:18-24.
Kenechukwu FC, Attama AA, Ibezim EC, Nnamani PO, Umeyor CE, Uronnachi EM, Momoh MA, Akpa PA. Tai-lor-made mucoadhesive lipid nanogel improves oromucosal antimycotic activity of encapsulated miconazole nitrate. Eur J Nanomed. 2017; 9(3-4):115-126.
Brange Jens. Gelenics of insulin, the physic-chemical and pharmaceutical aspect of insulin and insulin preparation, 15th Ed. Springer-Verlag, Berlin, Heidelberg, 1987. 1-81 p.
Wong CY, Martinez J, Dass CR. Oral delivery of insulin for treatmentof diabetes: Status quo, challenges and opportunities. J Pharm Pharmacol. 2016; 68:1093–1108.
Avadi MR, Sadeghi AMM, Naser M, Rassoul D. Ex vivoevaluation of insulin nanoparticles using chitosan and Arabic gum. ISRN Pharmaceut. 2011; 860109:6 pages.
Reddy M, Shanmugan MV, Rajesh K. Design and characterization of insulin nanoparticles for oral delivery. Int J Inn Pharm Res. 2012; 3(3):283-243.
Hamman JH. Chitosan-based polyelectrolyte complexes as potential carrier materials in drug delivery systems. Mar Drugs. 2010; 8:1305-1322.
Tai W and Gao X. Functional peptides for siRNA delivery. Adv Drug Rel Rev. 2016; 13:157–158.
Ofokansi KC and Kenechukwu FC. Formulation development and evaluation of drug release kinetics from colon targeted ibuprofen tablet based on Eudragit RL 100-chitosan interpolyelectrolyte complexes. ISRN Pharm. 2013; 2013:838403.
Momoh AM, Ossai EC, Omeje EC, Omenigbo OP, Kenechukwu FC, Ofokansi KO, Attama AA, Kunle OO. A new lipid-based oral delivery system of erythromycin for prolonged sustain release activity. J Mat Sci Eng. 2019; C97:245-254.