ENHANCEMENT OF THE RELEASE OF CURCUMIN BY THE FREEZE DRYING TECHNIQUE USING INULIN AND NEUSILIN AS CARRIERS
DOI:
https://doi.org/10.22159/ijap.2018v10i3.24429Keywords:
Curcumin, Inulin, Neusilin US2, Freeze-drying, Enhancement of solubilityAbstract
Objective: Curcumin (CUR), the active ingredient in turmeric has been proven to possess many therapeutic activities chiefly as anti-inflammatory and antioxidant. Unfortunately, CUR suffers from low bioavailability and dissolution due to its poor water solubility. The aim of this work was to enhance the dissolution of CUR by converting it into an amorphous form by freeze-drying and using different carriers.
Methods: Different solid dispersions of CUR with Inulin and Neusilin US2 at different ratios using the freeze-drying technique were prepared. The various prepared formulas were characterized using differential scanning calorimetry, X-ray diffraction studies, fourier transform infrared and scanning electron microscopy. Release studies, as well as stability studies of CUR from different formulas, were done.
Results: Formulation containing CUR, Inulin and Neusilin US2 at a ratio of 1:5:1 showed the highest CUR release during dissolution testing. The percent CUR release was 98% in comparison with that of 2% from the reference raw material. Physical stability testing showed that CUR remained in the amorphous state for 3 mo.
Conclusion: Inulin and Neusilin US2 combinations were found to be effective in enhancing the solubility and dissolution rate of CUR, and stabilizing the amorphous form in the prepared solid dispersion.
Downloads
References
Jurenka JS. Anti-inflammatory properties of curcumin, a major constituent of Curcuma longa: a review of preclinical and clinical research. Altern Med Rev 2009;14:141-53.
Banerjee S, Singh SK, Chowdhury I, Singh R. Combinatorial effect of curcumin with docetaxel modulates apoptotic and cell survival molecules in prostate cancer. Front Biosci (Elite Ed) 2017;9:235-45.
Bar Sela G, Epelbaum R, Schaffer M. Curcumin as an anti-cancer agent: a review of the gap between basic and clinical applications. Curr Med Chem 2010;17:190-7.
Moghadamtousi SZ, Kadir HA, Hassandarvish P, Tajik H, Abubakar S, Zandi K. A review on the antibacterial, antiviral, and antifungal activity of curcumin. Biomed Res Int 2014. Doi:10.1155/2014/186864.
Noorafshan A, Ashkani-Esfahani S. A review of therapeutic effects of curcumin. Curr Pharm Des 2013;19:2032-46.
Sharma S, Saraogi GK, Kumar V. Development of spectrophotometric methods for simultaneous determination of artesunate and curcumin in a liposomal formulation. Int J Appl Pharm 2015;7:18-21.
Abbas SH, Abdulridha MK, Najeb AA. The potential benefit of curcumin adjuvant therapy to the standard helicobacter pylori eradication therapy in patients with peptic ulcer disease. Asian J Pharm Clin Res 2017;10. Doi:10.22159/ajpcr.2017.v10i5.17462.
Shelat P, Mandowara VK, Gupta DG, Patel S. Formulation of curcuminoid loaded solid lipid nanoparticles in order to improve oral bioavailability. Int J Pharm Pharm Sci 2015;7:278-82.
Phongpradist R, Chaiyana W, Anuchapreeda S. Curcumin-loaded multi-valent ligands conjugated-nanoparticles for anti-inflammatory activity. Int J Pharm Pharm Sci 2015;7:203-8.
Kaur J, Bawa P, Rajesh SY, Sharma P, Ghai D, Jyoti J, et al. Formulation of curcumin nanosuspension using box-behnken design and study of the impact of drying techniques on its powder characteristics. Asian J Pharm Clin Res 2017;10:43.
Paradkar A, Ambike AA, Jadhav BK, Mahadik KR. Characterization of the curcumin-PVP solid dispersion obtained by spray drying. Int J Pharm 2004;271:281-6.
Hu L, Shi Y, Li JH, Gao N, Ji J, Niu F, et al. Enhancement of oral bioavailability of curcumin by a novel solid dispersion system. AAPS PharmSciTech 2015;16:1327-34.
Wang X, Jiang Y, Wang YW, Huang MT, Ho CT, Huang Q. Enhancing anti-inflammation activity of curcumin through O/W nanoemulsions. Food Chem 2008;108:419-24.
Allijn IE, Schiffelers RM, Storm G. Comparison of pharmaceutical nanoformulations for curcumin: enhancement of aqueous solubility and carrier retention. Int J Pharm 2016;506:407-13.
Sadeghi F, Ashofteh M, Homayouni A, Abbaspour M, Nokhodchi A, Garekani HA. Antisolvent precipitation technique: a very promising approach to crystallize curcumin in presence of polyvinyl pyrrolidon for solubility and dissolution enhancement. Colloids Surf B 2016;147:258-64.
Wong JJL, Yu H, Lim LM, Hadinoto K. A trade-off between solubility enhancement and physical stability upon simultaneous amorphization and nanonization of curcumin in comparison to amorphization alone. Eur J Pharm Sci 2018;114:356-63.
Donsì F, Wang Y, Li J, Huang Q. Preparation of curcumin sub-micrometre dispersions by high-pressure homogenization. J Agric Food Chem 2010;58:2848-53.
Teixeira CCC, Mendonça LM, Bergamaschi MM, Queiroz RHC, Souza GEP, Antunes LMG, et al. Microparticles containing curcumin solid dispersion: stability, bioavailability and anti-inflammatory activity. AAPS PharmSciTech 2016;17:252-61.
Raymond C Rowe PJs. Handbook of pharmaceutical Excipients. fifth edition ed. London; 2006.
Allgeier MC, Piper JL, Hinds J, Yates MH, Kolodsick KJ, Meury R, et al. Isolation and physical property optimization of an amorphous drug substance utilizing a high surface area magnesium aluminometasilicate (Neusilin((R)) US2). J Pharm Sci 2016;105:3105-14.
Gupta MK, Vanwert A, Bogner RH. Formation of physically stable amorphous drugs by milling with Neusilin. J Pharm Sci 2003;92:536-51.
Shah A, Serajuddin AT. Conversion of solid dispersion prepared by acid-base interaction into free-flowing and tabletable powder by using Neusilin(R) US2. Int J Pharm 2015;484:172-80.
Sruti J, Patra Ch N, Swain SK, Beg S, Palatasingh HR, Dinda SC, et al. Improvement in dissolution rate of cefuroxime axetil by using poloxamer 188 and neusilin US2. Indian J Pharm Sci 2013;75:67-75.
Khanfar M, Al-Nimry S. Stabilization and amorphization of lovastatin using different types of silica. AAPS PharmSciTech 2017;18:2358-67.
Amorij JP, Saluja V, Petersen AH, Hinrichs WL, Huckriede A, Frijlink HW. Pulmonary delivery of an inulin-stabilized influenza subunit vaccine prepared by spray-freeze drying induces systemic, mucosal humoral as well as cell-mediated immune responses in BALB/c mice. Vaccine 2007;25:8707-17.
Mensink MA, Frijlink HW, van der Voort Maarschalk K, Hinrichs WL. Inulin, a flexible oligosaccharide. II: a review of its pharmaceutical applications. Carbohydr Polym 2015;134:418-28.
Mensink MA, Frijlink HW, Van der Voort Maarschalk K, Hinrichs WL. Inulin, a flexible oligosaccharide I: review of its physicochemical characteristics. Carbohydr Polym 2015;130:405-19.
Visser MR, Baert L, Klooster G, Schueller L, Geldof M, Vanwelkenhuysen I, et al.,Inulin solid dispersion technology to improve the absorption of the BCS class IV drug TMC240. Eur J Pharm Biopharm 2010;74:233-8.
Fares MM, Salem MS. Dissolution enhancement of curcumin via curcumin-prebiotic inulin nanoparticles. Drug Dev Ind Pharm 2015;41:1785-92.
Fares MM, Salem MS, Khanfar M. Inulin and poly (acrylic acid) grafted inulin for dissolution enhancement and preliminary controlled release of poorly water-soluble Irbesartan drug. Int J Pharm 2011;410:206-11.
Rahman S, Telny T, Ravi T, Kuppusamy S. Role of surfactant and pH in the dissolution of curcumin. Indian J Pharm Sci 2009;71:139-42.
Li J, Lee IW, Shin GH, Chen X, Park HJ. Curcumin-eudragit(R) E PO solid dispersion: a simple and potent method to solve the problems of curcumin. Eur J Pharm Biopharm 2015;94:322-32.
Athira GK, Jyothi AN. Preparation and characterization of curcumin loaded cassava starch nanoparticles with improved cellular absorption. Int J Pharm Pharm Sci 2014;6:171-6.
Kojo Y, Matsunaga S, Suzuki H, Sato H, Seto Y, Onoue S. Improved oral absorption profile of itraconazole in hypochlorhydria by self-micellizing solid dispersion approach. Eur J Pharm Sci 2017;97:55-61.
Published
How to Cite
Issue
Section
