Formulation and In vivo Evaluation of Mucoadhesive Microspheres of Valsartan using Natural Gum
DOI:
https://doi.org/10.37285/ijpsn.2019.12.1.6Abstract
Microspheres containing valsartan were prepared by the ionotropic gelation method, using sodium alginate with other mucoadhesive polymers namely HPMC K 100M and Eudragit RL 100, Olibanum gum and Guar gum. The prepared batches were evaluated for different evaluation parameters. The in vitro drug release of optimized formulation M13 showed the sustained release of Valsartan up to 98.89 ± 5.25% within 12 h whereas marketed product displayed the drug release of 90.99 ± 4.96%. The release mechanism from microspheres followed the zero order and higuchi model (R2 = 0.988, 0.979) respectively. The optimized formulation (M13) shown % entrapment efficiency, % yield, swelling index and mucoadhesiveness of 98.18, 97.64, 97.42 and 96.18% respectively. From FTIR studies no incompatibility was found between drug and excipients. SEM confirmed that particles were of spherical in shape. Optimized formulation (M 13) was stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. From in vivo bioavailability studies, valsartan optimized formulation M13 exhibited sustained release in a controlled manner when compared with marketed product. Mean time to reach peak drug concentration (Tmax) was 4.00 ± 0.05 h and 3.00 ± 0.04 h for the optimized and marketed product respectively, while mean maximum drug concentration (Cmax) was 10.85 ± 0.03 ng/mL and 8.54 ± 0.01 ng/mL respectively. AUC0–∞ of optimized formulation was found to be 147.42 ± 1.16 ng.h/mL, when compared with marketed product of 119.15 ± 1.13 ng.h/mL, AUC values of optimized formulation were found to be significantly higher (p<0.05) than of marketed product. Valsartan muco-adhesive microspheres would be a promising drug delivery system, could play a potentially significant role in pharmaceutical drug delivery in the treatment of hypertension.
Downloads
Metrics
Keywords:
Valsartan, Ionotropic gelation method, Mucoadhesive microspheres, In vivo bioavailability
Downloads
Published
How to Cite
Issue
Section
References
Abdelbary G, Prinderre P, Eouani C, Joachim J, Reynier JP and Piccerelle P (2004). The preparation of orally disintegrating tablets using a hydrophilic waxy binder. Int J Pharm 278(2): 423-33.
Arifa Begum SK and Basava Raju D (2016). Formulation and Evaluation of Controlled Release Roxatidine Acetate HCl Mucoadhesive Microspheres: In-vivo Study. Research Journal of Pharmaceutical, Biological and Chemical Sciences 7(4): 1525-1532.
Armstrong NA and James KC (1996). Pharmaceutical Experimental Design and Interpretation. CRC Press, Informa Healthcare, New York.
Banker G.S and Rhodes (2002). C.T. Modern Pharmaceutics, 3rd ed. Marcel Dekker Inc, New York, pp 333-394.
Bindu MB, Zulkar NK, Ramalingam R, Ravindernath A, Kusum B, Naga MM and David B (2010). Formulation and evaluation of mucoadhesive microspheres of venlafaxine hydrochloride. Journal of Pharmaceutical Res 3(11): 2597-2600.
Caroter SJ (1986). Tutorial pharmacy Power flow and Compaction, 1st ed. CBS publishers and distributors, New Delhi, India, Chapter 19.
Charles RC and Robert ES (1997). Modern Pharmacology with Clinical Applications, 5th ed. Little Brown & Company, Boston, MA.
Chong BS and Mersfelder TL (2000). Entacapone. Ann Pharmacotherapy: 1056-65.
Fearnley J and Lees A (1994). Pathology of Parkinson's disease. In, Neurodegenerative Diseases: Calne DB, Saunders, Philadelphia, pp 545-554.
Gibb WR (1992). Neuropathology of Parkinson's disease and related syndromes. Neurol Clin 10: 361-376.
Haznedar MM, Buchsbaum MS, Hazlett EA, Shihabuddin L, New A and Siever LJ (2004). Cingulate gyrus volume and metabolism in the schizophrenia spectrum. Schizophr Res 71: 249-262.
Kumar S, Nagpal K, Singh SK and Mishra DN (2011). Improved Bioavailability through Floating Microspheres of Lovastatin. Daru 19: 57 -64.
Kurth MC, Adler CH, Hilaire MS, Singer C, Waters C, LeWitt P, Chernik DA, Dorflinger EE and Yoo K (1997). Tolcapone improves motor function and reduces levodopa requirement in patients with Parkinson's disease experiencing motor fluctuations. A multicenter double-blind, randomized placebo-controlled trial. Tolcapone Fluctuator Study Group I Neurology. Neurology 48(1): 81-87.
Lang AE and Lozano AM (1998). Parkinson's disease First of two parts. New Engl J Med 339:1044-1053
Liu Z, Lu W, Qian, Zhang X, Zeng, P and Pan J (2005). In Vitro and in Vivo Studies on Mucoadhesive Microspheres of Amoxicillin. J Control Release 102: 135-144.
Madhusudhan Malladi and Raju Jukanti (2016). Formulation development and evaluation of a novel bi-dependent clarithromycin gastroretentive drug delivery system using box-behnken design. J Drug Deliv Sci Technol 35:134-145.
Mankala SK, Korla AC and Gade S (2011). Study on effect of alginate and mucoadhesive polymers on drug release from Nateglinide loaded mucoadhesive microsphere. Journal of Pharmacy Research 4: 2732-40.
Najib J (2001). Entacapone a catechol-O-methyl-transferase inhibitor for the adjunctive treatment of Parkinson’s disease. Clin Ther 23(6): 802-32.
Pandya N, Pandya M and Bhaskar VH (2011). Preparation and In-vitro Characterization of Porous Carrier–Based Glipizide Floating Microspheres for Gastric Delivery. J Young Pharm 3: 97-104.
Parmar H, Bakliwal S, Gujarathi N and Pawar S (2010). Different methods of formulation and evaluation of mucoadhesive microsphere. International Journal of App Bio and Pharma Tech 3(3): 1157-1167.
Parul Trivedi, Verma A M L and Garud N (2008). Preparation and characterization of aceclofenac microspheres. Asian Journal of pharmaceutics: 110-115.
Rajput GC, Majumdar FD, Patel JK, Patel KN, Thakor RS, Patel BP and Rajgor NB (2010). Stomach Specific Mucoadhesive Tablets as Controlled Drug Delivery System-A Review Work. Int J Pharma & Bio Res (1): 30-41
Robinson RJ and Lee VH (2005). Controlled drug delivery Fundamentals and applications, 2nd ed. Marcel Dekker Inc , New York, pp 9-19.
Rockville (1980). The United States Pharmacopoeia XX/ National Formulary XV, 15th ed. US Pharmacopoeia Convention MD: 958-990.
Samya M El-Gizawy, Osama H Abdelmageed, Mahmoud A Omar, Sayed M Deryea and Ahmed M Abdel-Megied (2012). Development and Validation of HPLC Method for Simultaneous Determination of Amlodipine, Valsartan, Hydrochlorothiazide in Dosage Form and Spiked Human Plasma. Am J Analyt Chem 3: 422-430.
Senthil, Narayana Swamy V B, Ajit I, Galge Deepak S and Bhosale Rahul S (2011). Mucoadhesive Microspheres. International Journal of Research in Ayurveda & Pharmacy 2(1): 55- 59.
Sinha VR, Bansal K, Kaushik R, Kumria R and Trehan A (2004). Poly-epsilon-caprolactone microspheres and nanospheres an overview. Int J Pharm 18; 278(1): 1-23.
Ugwoke MI, Agu RU, Verbeke N and Kinget R (2005). Nasal mucoadhesive drug delivery. Background applications trends and future perspectives. Adv Drug Deliv Rev 57: 1640-65.
Vanshika Lumb, Manoj K Das, Neeru Singh, Vas Dev,Wajihullah Khan, and Yagya D (2011). Multiple Origins of Plasmodium falciparum Dihydropteroate Synthetase Mutant Alleles Associated with Sulfadoxine Resistance in India. Sharma Antimicrob Agents Chemother 55(6): 2813-2817.
