SUSTAINED RELEASE MUCOADHESIVE MICROCAPSULES OF RAMIPRIL BY IONIC GELATION TECHNIQUE: FORMULATION DESIGN, OPTIMIZATION AND CHARACTERIZATION
DOI:
https://doi.org/10.22159/ijpps.2017v9i2.12660Keywords:
Taguchi design, Box-Behnken design, Antihypertensive activity, Percentage bioadhesion, Sustained releaseAbstract
Objective: The major objective of the research work was to design, optimise and characterise sodium alginate based sustained release mucoadhesive microcapsules of ramipril by ionic gelation method.
Methods: An experimental set-up was designed to investigate the optimal combination of mucoadhesive polymers such as carbopol 974P, HPMC (K4M and K100M), Na CMC and chitosan and their drug compatibility with respect to reliabilities. Preliminary screening of the formulation variables was accomplished by Taguchi design followed by Box-Behnken design for systematic optimisation. The suitable mathematical model was selected, response surface analysis was performed and optimised formulation was chosen by numerical optimization and desirability function method. Characterization of the prepared microcapsules for several inherent properties like particle size, drug content, sphericity, entrapment efficiency, loose surface crystal study, swelling index, micromeritic properties, moisture content, in vitro drug release, mucoadhesive strength and in vivo antihypertensive activity was performed.
Results: Differential Scanning Calorimetry (DSC) thermograms and Fourier Transform Infra-Red (FT-IR) spectral studies revealed no incompatibility between the pure drug and selected polymers. The spherical nature of the prepared microcapsules was established by surface morphology studies.
Conclusion: The resultant sustained release mucoadhesive microcapsules of ramipril remained stable when subjected to stress conditions unveiling it as a better alternative delivery system with superior therapeutic efficacy.
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Modi SA, Gaikwad PD, Banker VH, Pawar SP. Sustained release drug delivery system a review. Int J Pharm Res Dev 2011;2:147-60.
Chen X, Wen H, Park K. Challenges and new technologies of oral controlled release, oral controlled release formulation design and drug delivery: Theory to Practice, Chapter-16; 2010. p. 257-7.
Rao R, Yadav A, kulkarni U. Formulation and evaluation of zero¬order release glipizide bilayer matrix tablets using natural and synthetic polymers. Int J Curr Pharm Res 2010;2:34-42.
Mohite PB, khanage SG, Harishchandre VS, Yogita S. Recent advances in microsponges drug delivery system. J Crit Rev 2016;3:9-16.
Tahami KL. Preparation, characterization, and in vitro release of ketoprofen loaded alginate microspheres. Int J Appl Pharm 2014;6:9-12.
Jagdale S, Dangat Y, Kuchekar B. Improvement of dissolution rate of ramipril by solid dispersion technique and development of buccal patch. Int J Pharm Pharm Sci 2012;4:309-18.
Martindale. The complete drug reference. 35th Edition; 2004. p. 1246.
Shafiq-un-Nabi S, Shakeel F, Talegaonkar S, Ali J, Baboota S, Ahuja A, et al. Formulation development and optimisation using nanoemulsion technique, A technical note. AAPS PharmSciTech 2007;8:E12-E17.
Kolli RG, Reddy VM, Patil CC, Kulkarni RV, Kalyani NV. Formulation and evaluation of matrix tablet of ramipril. Pharma Innovation J 2015;4:26-9.
Ekambaram P, Abdul HS. Formulation and evaluation of solid lipid nanoparticles of ramipril. J Young Pharm 2011;3:216-20.
Belgamwar V, Shah V, Surana SJ. Design and development of oral mucoadhesive multiparticulate system containing Atenolol, in vitro-in vivo characterization. Chem Pharm Bull 2010;58:1168-75.
Das MK, Maurya DP. Evaluation of diltiazem hydrochloride loaded mucoadhesive microspheres prepared by emulsification-internal gelation technique. Acta Poloniae Pharm Drug Res 2008;5:249-59.
Singh B, Kumar R, Ahuja N. Optimizing drug delivery systems using systematic Design of Experiments.†Part I, fundamental aspects. Crit Rev Ther Drug Carrier Syst 2004;22:27–105.
Singh B, Raza K, Beg S. Developing Optimized†drug products employing Designed†Experiments. Chem Ind Dig 2013;12:1-7.
Singh B, Ahuja N. Response surface optimisation of drug delivery systems. NK Jain. (Ed.) Progress in controlled and novel drug delivery systems. 1sted. CBS Publishers, New Delhi, India; 2004. p. 470-509.
Box GE, Behnken D. Some new three level designs for the study of quantitative variables. Technometrics 1960;2:455–75.
Taguchi G. A System of Experimental Design. Unipub/Kraus International Publications White Plains NY; 1987.
Lundstedt T, Seifert E, Abramo L, Thelin B, Nystrom A, Pettersen J, et al. Experimental design and optimisation. Chemom Intell Lab Syst 1998:42:3-40.
Doornbos CA, Haan PD. Optimization techniques in formulation and processing. In: J Swarbric K, JC Boylan. Eds. Encyclopedia of pharmaceutical technology, Marcel Dekker: New York; 1995. p. 77-160.
Kuehl RO. The design of experiments, statistical principles of research design and analysis; Duxbury/Thomson Learning; Pacific Grove CA; 2000.
Swain S, Behera A, Dinda SC, Patra CN, Jammula S, Beg S, et al. Formulation design, optimization and pharmacodynamic evaluation of sustained release mucoadhesive microcapsules of venlafaxine HCl. Indian J Pharm Sci 2014; 76:267-78.
Sharma HK, Pradhan SP, Sarangi B. Preparation and in vitro evaluation of enteric controlled release pantoprazole are loaded microbeads using natural mucoadhesive substance from Dillenia indica. Int J PharmTech Res 2010;2:542-51.
Swain S, Behera U, Beg S, Sruti J, Patro CN, Dinda SC, et al. Design and characterization of enteric-coated controlled release mucoadhesive microcapsules of rabeprazole sodium. Drug Dev Ind Pharm 2012;39:548-60.
Chowdary KP, Rao YS. Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release, a technical note. AAPS PharmSciTech 2003;4:E39.
Nayak AK, Hasnain MS, Beg S, Alam MI. Mucoadhesive beads of gliclazide, Design.; development and evaluation. Sci Asia 2010;36:319-25.
Loyd A, Nicholas GP. Pharmaceutical dosages forms and drug delivery systems: powders and granules. 9th ed. New Delhi, Wolters Kluwer/lippincott Williams and Wilkins; 2011. p. 184-202.
Nayak BS, Ghosh SK, Tripati K, Patro B. Preparation and characterization of famotidine microcapsule employing mucoadhesive polymers in combination to enhance gastro retention for oral delivery. Int J Pharm Sci 2009;1:112–20.
Tiwari SB, Murthy TK, Pai MR, Mehta PR, Chowdary PB. Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech 2003;4:1-6.
Arya RKK, Vijay JA, Singh R. Development and evaluation of gastro-resistant microspheres of pantoprazole. Int J Pharm Pharm Sci 2010;2:1575-80.
Albertini B, Passerini N, Sabatino MD, Vitali B, Brigidi P. Polymer–lipid-based mucoadhesive microspheres prepared by spray-congealing for the vaginal delivery of econazole nitrate. Eur J Pharm Sci 2009;36:591-601.
Swain S, Meher D, Patra CN, Jammula S, Dinda SC. Design and characterization of sustained release mucoadhesive microspheres of tolterodine tartrate. Curr Drug Delivery 2013;10:413-26.
Pouton CW. Effects of inclusion of a model drug on the performance of self-emulsifying formulations. J Pharm Pharmacol 1985;37:1–11.
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