Enhancing Oral Absorption of Orlistat through Gastroretentive Mucoadhesive Pellets: Formulation and Evaluation
Keywords:Bioavailability, Gastroretentive Drug Delivery Systems, Mucoadhesive, Orlistat, Swelling index
Aim: The aim of this study was to develop gastroretentive mucoadhesive pellets of Orlistat to improve its oral bioavailability and enhance its absorption.
Methods: Orlistat pellets were prepared using Hydroxy Propyl Methyl Cellulose (HPMC) K100M, Sodium Carboxy Methyl Cellulose (NaCMC), Carbopol 934P, and Polyvinyl Pyrrollidone (PVP) K30 in varying ratios. Physical characteristics of the tablets were evaluated, and compatibility studies were performed between Orlistat and the excipients. Swelling index, mucoadhesion strength and drug release were measured for each formulation. Drug release kinetics and stability studies were carried out.
Results: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 provided balanced release and mucoadhesion with F13 showing sustained release up to 16 hours. The calibration curve demonstrated a good linear relationship between Orlistat concentration and absorbance over the range of 10 to 50 ?g/ml. Swelling index increased with time and polymer concentration and mucoadhesion strength increased with polymer viscosity and concentration. Drug release from formulations containing HPMC K100M, NaCMC and Carbopol 934P were 12-14 hours, 10-12 hours and 8-11 hours, respectively. Combination polymers in F10-F13 provided balanced release and mucoadhesion, with F13 showing sustained release up to 16 hours. The drug release followed zero order kinetics with non-Fickian diffusion. Stability studies on the optimized F13 formulation showed no significant changes in appearance, hardness, mucoadhesion or drug release over 3 months.
Conclusion: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 improved the oral bioavailability and absorption of Orlistat. The study demonstrated the importance of compatibility studies and the use of calibration curves for quantitative analysis. The findings provide valuable insights into the development of drug delivery systems for poorly bioavailable drugs.
Lachman L, Schwartz JB. Herberta lie berman. Joseph L Kanig, The theory and Practice and industrial pharmacy, 2018: 293-345.
Banker GS. The Theory and Practice of Industrial Pharmacy. Journal of Pharmaceutical Sciences. 1970 Oct; 59(10):1531.
Kumar M, Kaushik D. An overview on various approaches and recent patents on gastroretentive drug delivery systems. Recent patents on drug delivery & formulation. 2018; 12(2): 84-92.
Kalpana GB, Bhaskar NV, Khan KAA, Prakash PR. Formulation, Optimization and Evaluation of Gastroretentive Alginate Beads of Ivacaftor by Using Factorial Design. Journal of Clinical and Pharmaceutical Research. 2021; 16-25.
Tripathi J, Thapa P, Maharjan R, Jeong SH. Current state and future perspectives on gastroretentive drug delivery systems. Pharmaceutics. 2019;11(4):193.
Kumar TH, Reddy KM, Rishika D, Kumar RP. Estimation of Orlistat by UV Spectrophotometric method. International Journal of Pharmaceutical Sciences and Research. 2011; 2(9): 2469.
Deshmukh MT, Mohite SK. Mucoadhesive Microsphere as a Drug Delivery System: A Review. Journal of Current Pharma Research. 2015; 5(3):1505.
Ahmed MG, Satish KBP, Kiran KGB. Formulation and evaluation of gastric-mucoadhesive drug delivery systems of captopril. Journal of Current pharmaceutical research. 2010; 2(1):26-32.
Hooda A. Gastroretentive drug delivery systems: A review of formulation approaches. The pharma innovation. 2012; 1(8): 79-107.
Fernandes GJ, Rathnanand M. Formulation optimization for gastroretentive drug delivery system of carvedilol cocrystals using design of experiment. Journal of Pharmaceutical Innovation. 2020; 15(3): 455-66.
Siraj S, Molvi KI, Nazim S. Various perspectives of Gastroretentive drug delivery System: A Review. American Journal of Advanced Drug Delivery. 2013; 1(4): 443-51.
Siddhapara M, Tikare V, Ramana MV, Sutariya B, Vaghasiya B. Gastroretentive drug delivery system: stomach specific mucoadhesive tablet. International research journal of Pharmacy. 2011; 2(12): 90-6.
Geldart D, Abdullah EC, Hassanpour A, Nwoke LC, Wouters I. Characterization of powder flowability using measurement of angle of repose. China Particuology. 2006; 4:104-7.
Almutairy BK, Khafagy ES, Alalaiwe A, Labrou NE, Aldawsari MF, Alshahrani SM, et al. Enhancing the Poor Flow and Tableting Problems of High Drug-Loading Formulation of Canagliflozin Using Continuous Green Granulation Process and Design-of-Experiment Approach. Pharmaceuticals. 2020; 13(12): 473.
Arora G, Malik K, Singh I, Arora S, Rana V. Formulation and evaluation of controlled release matrix mucoadhesive tablets of domperidone using Salvia plebeian gum. Journal of advanced pharmaceutical technology & research. 2011; 2(3):163.
Gudigennavar AS, Vijapur LS, Patil CC, Kulkarni RV. Development and evaluation of gastro-retentive drug delivery systems of cefuroxime axetil. Afr J Pharm Pharmacol. 2013; 7(20):1332-8.
Zate SU, Kothawade PI, Rathi MN, Shitole MH, Yewale CP, Gawande VS. Development and characterization of gastroretentive mucoadhesive tablets of venlafaxine hydrochloride. International Journal of Drug Delivery. 2010; 2(4): 299-303.
Sonani NG, Hiremath SP, Dasankoppa FS, Jamakandi VG, Sreenivas SA. Design and evaluation of gastroretentive mucoadhesive cephalexin tablets. Pharmaceutical development and technology. 2010; 15(2):178-83.
Mohanty C, Subrahmanyam KV. Design of controlled release mucoadhesive buccal tablets of Ivabradine HCl using sintering technique. Int J App Pharm. 2021 Jul 7;192-203.
Agarwal S, Murthy RSR. Effect of different polymer concentration on drug release rate and physicochemical properties of mucoadhesive gastroretentive tablets. Indian journal of pharmaceutical sciences. 2015; 77(6):705.
Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. Journal of pharmaceutical sciences. 1963; 52(12):1145-9.
Peppas NA. Analysis of Fickian and non-Fickian drug release from polymers. Pharmaceutica Acta Helvetiae. 1985; 60(4):110-1.
Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. International journal of pharmaceutics. 1983; 15(1): 25-35.
Patil S, Talele GS. Gastroretentive mucoadhesive tablet of lafutidine for controlled release and enhanced bioavailability. Drug delivery. 2015; 22(3): 312-9.
Sharma OP, Shah MV, Parikh DC, Mehta TA. Formulation optimization of gastroretentive drug delivery system for allopurinol using experimental design. Expert Opinion on Drug Delivery. 2015; 12(4):513-24.
Sandhya P, Kodali G, Fatima A. Formulation and in-vitro characterization of gastro retentive mucoadhesive tablets of Lovastatin. International Journal of Biological & Pharmaceutical Research. 2014; 5(1):71-7.
Ige PP, Gattani SG. Design, development and in vitro evaluation of swelling gastro retentive drug delivery system for type 2 diabetic patients. Latin American Journal of Pharmacy. 2011; 30.
Kremser C, Albrecht K, Greindl M, Wolf C, Debbage P, Bernkop-Schnürch A. In vivo determination of the time and location of mucoadhesive drug delivery systems disintegration in the gastrointestinal tract. Magnetic resonance imaging. 2008; 26(5):638-43.
Murphy CS, Pillay V, Choonara YE, du Toit LC. Gastroretentive drug delivery systems: current developments in novel system design and evaluation. Current drug delivery. 2009; 6(5):451-60.
Bansal M, Verma R, Mittal V, Kaushik D. Central Composite design for the development and evaluation of floating-mucoadhesive tablets of gliclazide. Current Drug Therapy. 2021; 16(1):113-23.
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