Development of Capsaicin Loaded Hydrogel Beads for In vivo Lipid Lowering Activities of Hyperlipidemic Rats

Author(s): Tapan Kumar Giri* , Tania Adhikary , Subhasis Maity .

Journal Name: Drug Delivery Letters

Volume 9 , Issue 2 , 2019

Become EABM
Become Reviewer

Graphical Abstract:


Objective: The presence of capsaicin in the diet has been revealed to enhance energy expenditure and it has been used in anti-obesity therapy. The present work investigated the potential antihyperlipidemic effect of capsaicin loaded hydrogel beads on hyperlipidemic rats. Hydrogels are three dimensional, hydrophilic, polymeric networks capable of imbibing large amounts of water or biological fluids.

Methods: Capsaicin loaded hydrogel beads were prepared by the ionotropic gelation method using Aluminium Chloride (AlCl₃) as a cross-linking agent. The characterization of hydrogel beads was carried out by X-ray Diffraction (XRD), Differential Scanning Calorimetry (DSC), and Scanning Electron Microscopic (SEM) analysis.

Results: The surface morphology revealed that the prepared beads were spherical in shape. XRD and DSC study of the hydrogel beads revealed that the drug was homogeneously dispersed in the hydrogel matrix. The beads showed pH sensitive behavior and when the medium pH was changed from 1.2 to 7.4, the capsaicin release was considerably increased. 100mg/kg body weight of Triton was injected intraperitoneally in rats to induce hyperlipidemia and it showed elevated levels of serum cholesterol and triglyceride. Capsaicin loaded hydrogel beads were administered to normal and hyperlipidemic rats for 7 days and the prepared hydrogel beads were significantly reduced high lipid profile in comparison to free capsaicin.

Conclusion: The results clearly demonstrated that hydrogel beads can be used as a potential carrier for delivery of capsaicin to reduce lipid profile.

Keywords: Capsaicin, hydrogel, gellan gum, swelling, cholesterol, obesity.

Giri, T.K.; Mukherjee, P.; Barman, T.K.; Maity, S. Nano-encapsulation of capsaicin on lipid vesicle and evaluation of their hepatocellular protective effect. Int. J. Biol. Macromol., 2016, 88, 236-243.
Giri, T.K.; Dey, B.; Maity, S. Preparation and characterization of nanoemulsome entrapped in enteric coated hydrogel beads for the controlled delivery of capsaicin to the colon. Curr. Drug Ther., 2018, 13, 98-105.
Hsu, C.L.; Yen, G.C. Effects of capsaicin on induction of apoptosis and inhibition of adipogenesis in 3T3-L1 cells. J. Agric. Food Chem., 2007, 55, 1730-1736.
Whiting, S.; Derbyshire, E.; Tiwari, B.K. Capsaicinoids and capsainoids: A potential role for weight management? A systematic review of evidence. Appetite, 2012, 59, 341-348.
Choi, S.E.; Kim, T.H.; Yi, S.A.; Hwanga, Y.C.; Hwanga, W.S.; Choe, S.J.; Han, S.J.; Kim, H.J.; Kim, D.J.; Kang, Y.; Lee, K.W. Capsaicin attenuates palmitate-induced expression of macrophage inflammatory protein 1 and interleukin protein 1 and interleukin 8 by increasing palmitate oxidation and reducing c-Jun activation in THP-1 (human acute monolytic leukemia cell) cells. Nutr. Res., 2011, 31, 468-478.
Akabori, H.; Yamamoto, H.; Tsuchihashi, H.; Mori, T.; Fujino, K.; Shimizu, T.; Endo, Y.; Tani, T. Transient receptor potential vanilloid 1 antagonist, capsazepine improves survival in a rat hemorrhagic shock model. Ann. Surg., 2007, 245, 964-970.
Josse, A.R.; Sherriffs, S.S.; Holwerda, A.M.; Andrews, R.; Staples, A.W.; Phillips, S.M. Effects of capsaicinoid ingestion on energy expenditure and lipid oxidation at rest and exercise. Nutr. Metab., 2010, 7, 65.
Lee, T.A.; Li, Z.; Zerlin, A.; Heber, D. Effects of dihydrocapsiate on adaptive and diet induced thermogenesis with a high protein very low calorie dietra randomized controlial. Nutr. Metab., 2010, 7, 78.
Lejeung, M.P.; Kovacs, E.M.; Westerterp-Plantenga, M.S. Effect of capsaicin on substrate oxidation and weight maintenance after modest body- weight loss in human subjects. Br. J. Nutr., 2003, 90, 651-659.
Ludy, M.J.; Mattes, R.D. The effects of hedonically acceptable red pepper do on thermogenesis and appetite. Physiol. Behav., 2011, 102, 251-258.
Lee, G.R.; Shin, M.K.; Yoon, D.J.; Kim, A.R.; Yu, R.; Park, N.H.; Han, I.S. Topical application of capsaicin reduces visceral adipose fat by affecting adipokine levels in high-fat diet-induced obese mice. Obesity , 2013, 21, 115-122.
Giri, T.K.; Pramanik, K.; Barman, T.K.; Maity, S. Nano-encapsulation of dietary phytoconstituent capsaicin on emulsome: Evaluation of anticancer activity through the measurement of liver oxidative stress in rats. Anticancer. Agents Med. Chem., 2017, 17, 1679-1688.
Giri, T.K.; Bhowmick, S.; Maity, S. Entrapment of capsaicin loaded nanoliposome in pH responsive hydrogel beads for colonic delivery. J. Drug Deliv. Sci. Technol., 2017, 39, 417-422.
Govindarajan, V.S.; Sathyanarayana, M.N. Capsicum-production, technology, chemistry and quality. Part V. Impact on physiology, pharmacology, nutrition and metabolism; Structure, pungency, pain and densitization sequences. Crit. Rev. Food Sci. Nutr., 1991, 29, 453-473.
Giri, T.K.; Verma, D.; Badwaik, H.R. Effect of aluminium chloride concentration on diltiazem hydrochloride release from pH-sentive hydrogel beads composed of hydrolyzed grafted k-carrageenan and sodium alginate. Curr. Chem. Biol., 2017, 11, 44-49.
Hoare, T.R.; Kohane, D.S. Hydrogels in drug delivery: Progress and challenges. Polymer , 2008, 49, 1993-2007.
Giri, T.K.; Pradhan, M.; Tripathi, D.K. Synthesis of graft copolymer of kappa-carrageenan using microwave energy and studies of swelling capacity, flocculation properties, and preliminary acute toxicity. Tur. J. Chem., 2016, 40, 283-295.
Gundamaraju, R.; Hwi, K.K.; Singla, R.K.; Vemuri, R.C.; Mulapalli, S.B. Antihyperlipidemic potential of Albiziaamara (Roxb) Boiv. bark against Triton X-100 induced hyperlipidemic condition in rats. Pharmacognosy Res., 2014, 6(4), 267-273.
Giri, T.K.; Thakur, A.; Tripathi, D.K. Biodegradable hydrogel bead of casein and modified xanthan gum for controlled delivery of theophylline. Curr. Drug Ther., 2016, 11, 150-162.
Mandal, S.; Kumar, S.S.; Krishnamoorthy, B.; Basu, S.K. Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods. Braz. J. Pharm. Sci., 2010, 46, 785-793.
Kulkarni, R.V.; Boppana, R.; Mohan, G.K.; Mutalik, S.; Kalyane, N.V. pH-responsive interpenetrating network hydrogel beads of poly(acrylamide)-g-carrageenan and sodium alginate for intestinal targeted drug delivery: Synthesis, in vitro and in vivo evaluation. J. Colloid Interface Sci., 2012, 367, 509-517.
Lin, C.C.; Metters, A.T. Hydrogels in controlled release formulations: network design and mathematical modeling. Adv. Drug Deliv. Rev., 2006, 58, 1379-1408.
Soppirnath, K.S.; Aminabhavi, T.M. Water transport and drug release study from cross-linked polyacrylamide grafted guar gum hydrogel microspheres for the controlled release application. Eur. J. Pharm. Biopharm., 2002, 53, 87-98.
Maiti, S.; Ranjit, S.; Mondol, S.; Ray, S.; Sa, B. Al+3 ion cross-linked and acetalated gellan hydrogel network beads for prolonged release of glipizide. Carbohydr. Polym., 2011, 85, 164-172.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2019
Page: [108 - 115]
Pages: 8
DOI: 10.2174/2210303109666190128151605
Price: $58

Article Metrics

PDF: 21