Abstract
To circumvent the solubility-related issues associated with Biopharmaceutics Classification System class II drugs, a novel porous carrier has been developed. In the present study, a process for preparation of porous starch (PS) is demonstrated. The process briefly comprises of translucent gel preparation followed by solvent replacement, drying, and sizing. Carbamazepine (CBZ) was used as a drug candidate to exhibit solubility enhancement potential of PS. PS and CBZ-loaded PS (CBZ-PS) systems were characterized with respect to IR, DSC, XRD, SEM, and dissolution kinetic studies. PS-CBZ was found to follow a Fickian behavior during dissolution. In vivo studies conducted in mice displayed a superior performance of CBZ-PS as compared to neat CBZ.
Similar content being viewed by others
REFERENCES
Hussain A, Rytting JH. Prodrug approach to enhancement of rate of dissolution of allopurinol. J Pharm Sci. 1974;63(5):798–9.
Alonzo DE, Gao Y, Zhou D, Mo H, Zhang GG, Taylor LS. Dissolution and precipitation behavior of amorphous solid dispersions. J Pharm Sci. 2011;100(8):3316–31.
Jadhav GS, Vavia PR. Physicochemical in silico and in-vivo evaluation of danazole-β cyclodextrin complex. Int J Pharm. 2008;2008(352):5–16.
Ambrogi V, Perioli L, Pagano C, Marmottini F, Ricci M, Sagnella A, et al. Use of SBA-15 for furosemide oral delivery enhancement. Eur J Pharm Sci. 2012;46(1–2):43–8.
Tatavarti AS, Hoag SW. Microenvironmental pH modulation based release enhancement of a weakly basic drug from hydrophilic matrices. J Pharm Sci. 2006;95(7):1459–68.
Murdande SB, Pikal MJ, Shanker RM, Bogner RH. Solubility advantage of amorphous pharmaceuticals: II. Application of quantitative thermodynamic relationships for prediction of solubility enhancement in structurally diverse insoluble pharmaceuticals. Pharm Res. 2010;27(12):2704–14.
Meer TS, Sawant KP, Amin PD. Liquid anti solvent precipitation process for solubility modulation of bicalutamide. Acta Pharma. 2011;61(4):435–45.
Moffat AC, Osselton MD, Widdop Clarke B. Analysis of drugs and poisons, vol. II. London: Pharmaceutical Press; 2004. p. 747–49.
Ambrogi V, Perioli L, Marmottini F, Accorsi O, Pagano C, Ricci M, et al. Role of mesoporous silicates on carbamazepine dissolution rate enhancement. Microporous Mesoporous Mater. 2008;113(1–3):445–52.
Achumecher GE. Therapeutic drug monitoring. New York: Appleton and Lange; 1995. p. 345–95.
Tayel SA, Soliman II, Louis D. Improvement of dissolution properties of carbamazepine through application of liquisolid tablet technique. Eur J Pharm Biopharm. 2008;69(1):342–7.
Wang Z, Chen B, Quan G, Li F, Wu Q, Dian L, et al. Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica. Int J Nanomedicine. 2012;7(1):5807–18.
Wang M, Rutledge GC, Myerson AS, Trout BL. Production and characterization of carbamazepine nanocrystals by electrospraying for continuous pharmaceutical manufacturing. J Pharm Sci. 2012;101(3):1178–88.
Xu L, Ming L, Zhefei G, Lin H, Xin F, Chuanbin W. Improving the chemical stability of amorphous solid dispersion with cocrystal technique by hot melt extrusion. Pharm Res. 2012;29(3):806–17.
Rowe RC, Shesky PJ, Quinn ME. Handbook of pharmaceutical excipients. 6th ed. London: Pharmaceutical Press; 2009. p. 685–90.
Uthumporn U, Zaidul ISM, Karim AA. Hydrolysis of granular starch at sub-gelatinization temperature using a mixture of amylolytic enzymes. Food Bioprod Process. 2010;88(1):47–54.
Guan JJ, Hanna MA. Extruding foams from corn starch acetate and native corn starch. Biomacromolecules. 2004;5(6):2329–39.
Torres FG, Boccaccini AR, Troncoso OP. Microwave processing of starch based porous structures for tissue engineering scaffolds. J Appl Polym Sci. 2007;103(2):1332–9.
Manoi K, Rizvi SSH. Physicochemical characteristics of phosphorylated cross-linked starch produced by reactive supercritical fluid extrusion. Carbohydr Polym. 2010;81(3):687–94.
Wu C, Wang Z, Zhi Z, Jiang T, Zhang J, Wang S. Development of biodegradable porous starch foam for improving oral delivery of poorly water soluble drugs. Int J Pharm. 2011;403(1–2):162–9.
The United States Pharmacopeia (USP29). 29th ed. Rockville, MD: United States Pharmacopeial Convention Inc.; 2006.
Ahuja N, Katare OP, Singh B. Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. Eur J Pharm Biopharm. 2007;65(1):26–38.
Korsemeyer RW, Gurney R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15(1):25–35.
Grzesiak AL, Lang M, Kim K, Matzger AJ. Comparison of the four anhydrous polymorphs of carbamazepine and the crystal structure of form I. J Pharm Sci. 2003;92(11):2260–71.
Zhang B, Cui D, Liu M, Gong H, Huang Y, Han F. Corn porous starch: preparation, characterization and adsorption property. Int J Biol Macromol. 2012;50(1):250–6.
Vasko PD, Blackwell J, KoenigInfrared JL. Raman spectroscopy of carbohydrates: part II: normal coordinate analysis of α-D-glucose. Carbohydr Res. 1972;23(3):407–16.
Cael SJ, Koenig JL, Blackwell J. Infrared and Raman spectroscopy of carbohydrates: part III: Raman spectra of the polymorphic forms of amylose. Carbohydr Res. 1973;29(1):123–34.
Dinunzio JC, Miller DA, Yang W, Mcginity GW, Williams RO. Amorphous compositions using concentration enhancing polymers for improved bioavailability of itraconazole. Mol Pharm. 2008;5(6):968–80.
Chan L, Caixia L, Yuan L, Jian-Feng C. Formation of bicalutamide nanodispersion for dissolution rate enhancement. Int J Pharm. 2011;404(1–2):257–63.
Corrigan OI, Holohan EM. Amorphous spray-dried hydroflumethiazide-polyvinylpyrrolidone systems: physicochemical properties. J Pharm Pharmacol. 1984;36(4):217–21.
Clinckers R, Smolders I, Meurs A, Ebinger G, Michotte Y. Quantitative in vivo microdialysis study on the influence of multidrug transporters on the blood–brain barrier passage of oxcarbazepine: concomitant use of hippocampal monoamines as pharmacodynamic markers for the anticonvulsant activity. J Pharmacol Exp Ther. 2005;314(2):725–31.
Hoogerkamp A, Vis PW, Danhof M, Voskuyl RA. Characterization of the pharmacodynamics of several antiepileptic drugs in a direct cortical stimulation model of anticonvulsant effect in the rat. J Pharmacol Exp Ther. 1994;269(2):521–8.
Paschoa OED, Mandema JW, Voskuyl RA, Danhof M. Pharmacokinetic-pharmacodynamic modeling of the anticonvulsant and electroencephalogram effects of phenytoin in rats. J Pharmacol Exp Ther. 1998;284(2):460–6.
Qian D, Chang PR, Ma X. Preparation of controllable porous starch with different starch concentrations by the single or dual freezing process. Carbohydr Polym. 2011;86(3):1181–6.
Qian D, Anderson DP, Ma X. Preparation and properties of the succinic ester of porous starch. Carbohydr Polym. 2012;88(2):604–8.
ACKNOWLEDGMENTS
The authors would like to thank University Grants Commission, Government of India, for their financial support.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Ali, M.T., Fule, R., Sav, A. et al. Porous Starch: a Novel Carrier for Solubility Enhancement of Carbamazepine. AAPS PharmSciTech 14, 919–926 (2013). https://doi.org/10.1208/s12249-013-9985-6
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1208/s12249-013-9985-6