FORMULATION AND OPTIMIZATION OF CURCUMIN SOLID DISPERSION PELLETS FOR IMPROVED SOLUBILITY

Authors

  • SANJEEVANI DESHKAR Department of Pharmaceutics, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, 411018, Maharashtra, India
  • ARUN SATPUTE Department of Pharmaceutics, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, 411018, Maharashtra, India

DOI:

https://doi.org/10.22159/ijap.2020v12i2.34846

Keywords:

Curcumin, Poloxamer, Solid dispersion, Pluronic, Factorial design

Abstract

Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility.

Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution.

Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets.

Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.

Downloads

Download data is not yet available.

References

Girish C, Koner BC, Jayanthi S, Ramachandra Rao K, Rajesh B, Pradhan SC. Hepatoprotective activity of picroliv, curcumin and ellagic acid compared to silymarin on paracetamol-induced liver toxicity in mice. Fundam Clin Pharmacol 2009;23:735–45.

Shehzad A, Rehman G, Lee YS. Curcumin in inflammatory diseases. BioFactors 2013;39:69–77.

Gangwar RK, Tomar GB, Dhumale VA, Zinjarde S, Sharma RB, Datar S. Curcumin conjugated silica nanoparticles for improving bioavailability and its anticancer applications. J Agric Food Chem 2013;61:9632–7.

Pulido Moran M, Moreno Fernandez J, Ramirez Tortosa C, Ramirez Tortosa MC. Curcumin and health. Molecules 2016;21:1–22.

Anand P, Kunnumakkara AB, Newman RA, Aggarwal BB. Bioavailability of curcumin: problems and promises. Mol Pharmaceutics 2007;4:807–18.

Bikiaris DN. Solid dispersions, Part II: New strategies in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs. Expert Opin Drug Delivery 2011;8:1663–80.

Xu D, Wang S, Jin J, Mei X, Xu S. Dissolution and absorption researches of curcumin in solid dispersions with the polymers PVP. Asian J Pharmacodynamics Pharmacokinetics 2006;6:343–9.

Tripodo G, Pasut G, Trapani A, Mero A, Lasorsa FM, Chlapanidas T, et al. Inulin-d-α-tocopherol succinate (INVITE) nanomicelles as a platform for effective intravenous administration of curcumin. Biomacromolecules 2015;16:550–7.

Li J, Lee IW, Shin GH, Chen X, Park HJ. Curcumin-eudragit® EPO solid dispersion: a simple and potent method to solve the problems of curcumin. Eur J Pharm Biopharm 2015;94:322–32.

Dewangan AK, Mazumder S, Perumal Y, Chopra K, Mazumder S. Preparation, characterization and anti-inflammatory effects of curcumin loaded carboxymethyl cellulose acetate butyrate nanoparticles on adjuvant induced arthritis in rats. J Drug Delivery Sci Technol 2017;41:269–79.

Fan N, He Z, Ma P, Wang X, Li C, Sun J, et al. Impact of HPMC on inhibiting crystallization and improving permeability of curcumin amorphous solid dispersions. Carbohydr Polym 2018;181:543–50.

Jagadeesan R, Radhakrishnan M. Novel approaches in the preparation of solid dispersion on solubility: a review. Int J Pharm Pharm Sci 2013;5:1000–4.

Seo SW, Han HK, Chun MK, Choi HK. Preparation and pharmacokinetic evaluation of curcumin solid dispersion using solutol ® HS15 as a carrier. Int J Pharm 2012;424:18–25.

Sharma A, Jain CP. Solid dispersion: a promising technique to enhance solubility of poorly water-soluble drug. Int J Drug Delivery 2011;1:149–70.

Parikh A, Kathawala K, Song Y, Zhou XF, Garg S. Curcumin-loaded self-nanomicellizing solid dispersion system: part I: development, optimization, characterization, and oral bioavailability. Drug Delivery Transl Res 2018;8:1389–405.

Radjaram A, Fuad Hafid A, Setyawan D. Dissolution enhancement of curcumin by hydroxypropyl-β-cyclodextrin complexation. Int J Pharm Pharm Sci 2013;5:401–5.

Kurmi R, Mishra DK, Jain DK. Solid dispersion: a novel means of solubility enhancement. J Critical Rev 2016;3:1–8.

Saffoon N, Uddin R, Huda NH, Sutradhar KB. Enhancement of oral bioavailability and solid dispersion: a review. J Appl Pharm Sci 2011;1:13–20.

Patil AN, Shinkar DM, Saudagar RB. Review article: solubility enhancement by solid dispersion. Int J Curr Pharm Res 2017;9:15-8.

Pratap Singh D, Joshi Hanumanthachar K, Bharathi G. Enhancement of aqueous solubility of curcumin by solid dispersion technology. World J Pharm Pharm Sci 2015;2:4109–20.

Li B, Konecke S, Wegiel LA, Taylor LS, Edgar KJ. Both solubility and chemical stability of curcumin are enhanced by solid dispersion in cellulose derivative matrices. Carbohydr Polym 2013;98:1108–16.

Setthacheewakul S, Mahattanadul S, Phadoongsombut N, Pichayakorn W, Wiwattanapatapee R. Development and evaluation of self-microemulsifying liquid and pellet formulations of curcumin, and absorption studies in rats. Eur J Pharm Biopharm 2010;76:475–85.

Fousteris E, Tarantili PA, Karavas E, Bikiaris D. Poly(vinyl pyrrolidone)-poloxamer-188 solid dispersions prepared by hot melt extrusion: thermal properties and release behavior. J Therm Anal Calorim 2013;113:1037–47.

Najmuddin M, Khan T, Majed A, Shelar S, Patel V. Enhancement of dissolution rate of ketoconazole by solid dispersion technique. Int J Pharm Pharm Sci 2010;2:132–6.

Gangurde AB, Kundaikar HS, Javeer SD, Jaiswar DR, Degani MS, Amin PD. Enhanced solubility and dissolution of curcumin by a hydrophilic polymer solid dispersion and its insilico molecular modeling studies. J Drug Delivery Sci Technol 2015;29:226–37.

Boddu P, Cherakapu VL, Ponukumati UD. Application of solid dispersion technique in solubility and dissolution rate enhancement of nateglinide. Asian J Pharm Clin Res 2017;10:231-8.

Wakeham S, Heung S, Lee J, Sadowski CA. Beyond equality: providing equitable care for persons with disabilities. Can Pharm J 2017;150:251–8.

United States Pharmacopeia and National Formulary (USP 30-NF 25). Rockville, MD: United States Pharmacopeial Convention; 2007.

Bharti VP, Attal VR, Munde AV, Birajdar AS, Bais S. Strategies to enhance solubility and dissolution of a poorly water soluble drug. J Innovations Pharm Biol Sci 2015;2:481–94.

Paradkar A, Ambike AA, Jadhav BK, Mahadik KR. Characterization of Cu-PVP solid dispersion obtained by spray drying. Int J Pharm 2004;271:281-6.

Published

07-03-2020

How to Cite

DESHKAR, S., & SATPUTE, A. (2020). FORMULATION AND OPTIMIZATION OF CURCUMIN SOLID DISPERSION PELLETS FOR IMPROVED SOLUBILITY. International Journal of Applied Pharmaceutics, 12(2), 36–46. https://doi.org/10.22159/ijap.2020v12i2.34846

Issue

Section

Original Article(s)