Formulation and Characterization of Solid Dispersion Containing Capsaicin for the Treatment of Diabetes

Author(s): Tapan Kumar Giri*, Payel Roy, Subhasis Maity

Journal Name: Current Drug Therapy

Volume 15 , Issue 3 , 2020

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Graphical Abstract:


Background: Chili peppers are widely used in many cuisines as a spice, and capsaicin is the main component. It has been reported that capsaicin acts as an antihyperglycemic agent. However, it shows poor aqueous solubility and bioavailability.

Objective: The is to enhance the aqueous solubility and antihyperglycemic activity of capsaicin through solid dispersion formulation.

Methods: Solid dispersions were prepared by the solvent evaporation method using polyethylene glycol 6000 (PEG 6000) as a hydrophilic carrier. Polymer-drug miscibility and drug crystallinity were characterized through the differential thermal analysis and X-ray powder patterns analysis. Solid dispersions were evaluated for solubility, in vitro drug dissolution and in vivo animal study in rats.

Results: Results of x-ray powder patterns analysis showed a considerable reduction of drug crystallinity in solid dispersion. Differential thermal analysis result revealed a complete disappearance of capsaicin melting onset temperature in solid dispersion. From the phase solubility data, it was observed that the aqueous solubility of capsaicin was increased with increasing concentration of PEG 6000. Solid dispersion formulation showed considerable enhancement of in vitro release of drugs in comparison to pure capsaicin. In vivo animal study in rats shows that the solid dispersion containing capsaicin significantly reduced the blood glucose level in comparison to the free capsaicin.

Conclusion: Higher anti-hyperglycemic effect of capsaicin loaded solid dispersion in comparison to the pure drug may be due to the enhancement of aqueous solubility of capsaicin. Thus, the solid dispersion of capsaicin showed a simple approach for capsaicin delivery with improved antidiabetic activity.

Keywords: Solid dispersion, capsaicin, in vitro dissolution rate, phase solubility, solubility enhancement, diabetes.

Guariguata L, Whiting DR, Hambleton I, Beagley J, Linnenkamp U, Shaw JE. Global estimates of diabetes prevalence for 2013 and projections for 2035. Diabetes Res Clin Pract 2014; 103(2): 137-49.
[] [PMID: 24630390]
Réggami Y, Berredjem H, Cheloufi H, Berredjem M, Bouzerna N. Antihyperglycemic and antidiabetic effects of Ethyl (S)-2-(1-cyclohexylsulfamide carbamoyloxy) propanoate in streptozotocin-induced diabetic Wistar rats. Eur J Pharmacol 2016; 779: 122-30.
[] [PMID: 26970184]
Holstein A, Beil W. Oral antidiabetic drug metabolism: pharmacogenomics and drug interactions. Expert Opin Drug Metab Toxicol 2009; 5(3): 225-41.
[] [PMID: 19331589]
Zhang Y, Hu T, Zhou H, Zhang Y, Jin G, Yang Y. Antidiabetic effect of polysaccharides from Pleurotus ostreatus in streptozotocin-induced diabetic rats. Int J Biol Macromol 2016; 83: 126-32.
[] [PMID: 26627601]
Panunti B, Jawa AA, Fonseca VA. Mechanisms and therapeutic targets in type 2 diabetes mellitus. Drug Discov Today Dis Mech 2004; 1: 151-7.
Zhang W, Zheng L, Zhang Z, Hai CX. Protective effect of a water-soluble polysaccharide from Salvia miltiorrhiza Bunge on insulin resistance in rats. Carbohydr Polym 2012; 89(3): 890-8.
[] [PMID: 24750877]
Pradhan S, Sinha C. High throughput screening based highly potent sulfonylbenzamide anti-diabetic drug. Curr Drug Ther 2018; 13(2): 162-73.
Wu X, Chen K, Williams KJ. The role of pathway-selective insulin resistance and responsiveness in diabetic dyslipoproteinemia. Curr Opin Lipidol 2012; 23(4): 334-44.
[] [PMID: 22617754]
Bajpeyi S, Pasarica M, Moro C, et al. Skeletal muscle mitochondrial capacity and insulin resistance in type 2 diabetes. J Clin Endocrinol Metab 2011; 96(4): 1160-8.
[] [PMID: 21307136]
Liu Z, Li W, Li X, et al. Antidiabetic effects of malonyl ginsenosides from Panax ginseng on type 2 diabetic rats induced by high-fat diet and streptozotocin. J Ethnopharmacol 2013; 145(1): 233-40.
[] [PMID: 23147499]
Giri TK, Pramanik K, Barman TK, 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(12): 1669-78.
[PMID: 28425858]
Giri TK, Bhowmick S, Maity S. Entrapment of capsaicin loaded nanoliposome in pH responsive hydrogel beads for colonic delivery. J Drug Deliv Sci Technol 2017; 39: 417-22.
Giri TK, Mukherjee P, Barman TK, Maity S. Nano-encapsulation of capsaicin on lipid vesicle and evaluation of their hepatocellular protective effect. Int J Biol Macromol 2016; 88: 236-43.
[] [PMID: 27032489]
Suri A, Szallasi A. The emerging role of TRPV1 in diabetes and obesity. Trends Pharmacol Sci 2008; 29(1): 29-36.
[] [PMID: 18055025]
Razavi R, Chan Y, Afifiyan FN, et al. TRPV1+ sensory neurons control beta cell stress and islet inflammation in autoimmune diabetes. Cell 2006; 127(6): 1123-35.
[] [PMID: 17174891]
Akiba Y, Kato S, Katsube K, et al. Transient receptor potential vanilloid subfamily 1 expressed in pancreatic islet beta cells modulates insulin secretion in rats. Biochem Biophys Res Commun 2004; 321(1): 219-25.
[] [PMID: 15358238]
Kang JH, Tsuyoshi G, Le Ngoc H, et al. Dietary capsaicin attenuates metabolic dysregulation in genetically obese diabetic mice. J Med Food 2011; 14(3): 310-5.
[] [PMID: 21332406]
Kang JH, Goto T, Han IS, Kawada T, Kim YM, Yu R. Dietary capsaicin reduces obesity-induced insulin resistance and hepatic steatosis in obese mice fed a high-fat diet. Obesity 2010; 18(4): 780-7.
[] [PMID: 19798065]
Giri TK, Thakur A, Tripathi DK. Biodegradable hydrogel bead of casein and modified xanthan gum for controlled delivery of theophylline. Curr Drug Ther 2016; 11: 150-62.
Giri TK, 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.
Pawar HA, Shinde PR. Enhancement of solubility of lutein by solid dispersion technique and development of its stable orodispersible film formulation. Curr Drug Ther 2018; 13: 140-51.
Giri TK, Verma D, Badwaik HR. 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: 44-9.
Giri TK, Vishwas S, Tripathi DK. Synthesis of grafted locust bean gum using vinyl monomer and studies of physicochemical properties and acute toxicity. Nat Prod J 2016; 6: 1-9.
Giri TK, Pradhan M, Tripathi DK. Synthesis of graft copolymer of kappa-carrageenan using microwave energy and studies of swelling capacity, flocculation properties, and preliminary acute toxicity. Turk J Chem 2016; 40: 283-95.
Giri TK, Verma U, Tripathi DK. Effect of adsorption parameters on biosorption of Zn++ ions from aqueous solution by graft copolymer of locust bean gum and polyacrylamide. Indian J Chem Technol 2016; 23: 93-103.
Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001; 13(2): 123-33.
[] [PMID: 11297896]
Mura P, Faucci MT, Manderioli A, Bramanti G, Parrini P. Thermal behavior and dissolution properties of naproxen from binary and ternary solid dispersions. Drug Dev Ind Pharm 1999; 25(3): 257-64.
[] [PMID: 10071817]
Valleri M, Mura P, Maestrelli F, Cirri M, Ballerini R. Development and evaluation of glyburide fast dissolving tablets using solid dispersion technique. Drug Dev Ind Pharm 2004; 30(5): 525-34.
[] [PMID: 15244088]
Palmieri GF, Cantalamessa F, Di Martino P, Nasuti C, Martelli S. Lonidamine solid dispersions: in vitro and in vivo evaluation. Drug Dev Ind Pharm 2002; 28(10): 1241-50.
[] [PMID: 12476870]
Zhai X, Li C, Lenon GB, Xue CCL, Li W. Preparation and characterisation of solid dispersions of tanshinone IIA, cryptotanshinone and total tanshinones. Asian J Pharm Sci 2017; 12(1): 85-97.
[] [PMID: 32104317]
Shamsipur M, Pourmortazavi SM, Beigi AA, Heydari R, Khatibi M. Thermal stability and decomposition kinetic studies of acyclovir and zidovudine drug compounds. AAPS PharmSciTech 2013; 14(1): 287-93.
[] [PMID: 23299688]
Martin A, Bustamante P, Chun AHC. Physical Pharmacy. Lippincott Williams & Wilkins 2001; p. p331.
Craig DQM, Newton JM. The dissolution of nortriptyline HCl from polyethylene glycol solid dispersions. Drug Dev Ind Pharm 1985; 11: 697-724.

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Article Details

Year: 2020
Published on: 13 October, 2020
Page: [219 - 225]
Pages: 7
DOI: 10.2174/1574885514666190916152432
Price: $65

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