Solid dispersion as a formulation strategy: A mini review
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Keywords

solid dispersion
solubility
drug delivery systems
amorphous
crystalline
review

How to Cite

Patel, P. (2017). Solid dispersion as a formulation strategy: A mini review. International Journal of Chemical and Life Sciences, 6(6), 2039-2045. https://doi.org/10.21746/ijcls.2017.6.1

Abstract

Oral route has been the most preferred route for administration of drug.  However, in recent years majority of new drug candidates exhibit poor aqueous solubility for oral administration and hence pose a challenge for the formulation scientist [1].   Dissolution and/or permeation across the gastrointestinal membrane are the rate limiting step for oral absorption of drugs.  Majority of the drugs belong to Class II of Biopharmaceutical Classification System (BCS).  For these drugs, dissolution is the sole rate limiting step in oral absorption [2]. The current review lightens the advantages of the solid dispersion and discusses the production techniques, types of solid dispersion, and methods to choose a suitable carrier. Also, the common characterization techniques are explained. This mini review would help the readers understand the overall concept of solid dispersion as a drug delivery system.
https://doi.org/10.21746/ijcls.2017.6.1
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References

Dannenfelser R-M, He H, Joshi Y, Bateman S, Serajuddin ATM. Development of clinical dosage forms for a poorly water soluble drug I: Application of polyethylene glycol–polysorbate 80 solid dispersion carrier system. J Pharm Sci [Internet]. 2004 May;93(5):1165–75. Available from: http://www.ncbi.nlm.nih.gov/pubmed/15067693

Amidon GL, Lennernäs H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res [Internet]. 1995 Mar;12(3):413–20. Available from: http://www.ncbi.nlm.nih.gov/pubmed/7617530

Jain S, Patel N, Shah MK, Khatri P, Vora N. Recent Advances in Lipid-Based Vesicles and Particulate Carriers for Topical and Transdermal Application. J Pharm Sci [Internet]. 2017 Feb 1;106(2):423–45. Available from: http://www.sciencedirect.com/science/article/pii/S0022354916417715

Shah MK, Madan P, Lin S. Elucidation of intestinal absorption mechanism of carvedilol-loaded solid lipid nanoparticles using Caco-2 cell line as an in-vitro model. Pharm Dev Technol [Internet]. 2015 Oct 3;20(7):877–85. Available from: http://www.tandfonline.com/doi/full/10.3109/10837450.2014.938857

MK Shah. Solid Lipid Nanoparticles (SLN) for Oral Drug Delivery: An Overview. J Nanomed Nanosci [Internet]. 2017; Available from: http://gavinpublishers.com/wp-content/uploads/2017/06/JNAN-109.pdf

Reddy Y. A Brief Review on Polymeric Nanoparticles for Drug Delivery and Targeting. jmedpharm.com [Internet]. Available from: http://www.jmedpharm.com/index.php?journal=JMPI&page=article&op=view&path%5B%5D=77

Leuner C, Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm [Internet]. 2000 Jul 3;50(1):47–60. Available from: http://www.sciencedirect.com/science/article/pii/S093964110000076X

Serajuddin AT. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J Pharm Sci [Internet]. 1999 Oct;88(10):1058–66. Available from: http://www.ncbi.nlm.nih.gov/pubmed/10514356

Craig DQM. The mechanisms of drug release from solid dispersions in water-soluble polymers. Int J Pharm [Internet]. 2002 Jan 14;231(2):131–44. Available from: http://www.ncbi.nlm.nih.gov/pubmed/11755266

Chiou WL, Riegelman S. Pharmaceutical Applications of Solid Dispersion Systems. J Pharm Sci [Internet]. 1971 Sep 1;60(9):1281–302. Available from: http://linkinghub.elsevier.com/retrieve/pii/S0022354915380850

Huang Y, Dai W-G. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharm Sin B [Internet]. 2014 Feb 1;4(1):18–25. Available from: http://www.sciencedirect.com/science/article/pii/S2211383513000968

Vasconcelos T, Sarmento B, Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today [Internet]. 2007 Dec;12(23–24):1068–75. Available from: http://www.ncbi.nlm.nih.gov/pubmed/18061887

May DR, Kolthoff IM. Studies on the Aging of Precipitates and Coprecipitation. XL. The Solubility of Lead Chromate as a Function of the Particle Size. J Phys Colloid Chem [Internet]. 1948 May;52(5):836–54. Available from: http://pubs.acs.org/doi/abs/10.1021/j150461a009

Doherty C, York P. Accelerated Stability of an X-Ray Amorphous Frusemide-Polyvinylpyrrolidone Solid Dispersion. Drug Dev Ind Pharm [Internet]. 1989 Jan 20;15(12):1969–87. Available from: http://www.tandfonline.com/doi/full/10.3109/03639048909052513

Konno H, Taylor LS. Influence of Different Polymers on the Crystallization Tendency of Molecularly Dispersed Amorphous Felodipine. J Pharm Sci [Internet]. 2006 Dec;95(12):2692–705. Available from: http://www.ncbi.nlm.nih.gov/pubmed/16892209

Taylor LS, Zografi G. Spectroscopic Characterization of Interactions Between PVP and Indomethacin in Amorphous Molecular Dispersions. Pharm Res [Internet]. 1997;14(12):1691–8. Available from: http://link.springer.com/10.1023/A:1012167410376

Janssens S, Van den Mooter G. Review: physical chemistry of solid dispersions. J Pharm Pharmacol [Internet]. 2009 Dec 1;61(12):1571–86. Available from: http://doi.wiley.com/10.1211/jpp.61.12.0001

Sethia S, Squillante E. Physicochemical Characterization of Solid Dispersions of Carbamazepine Formulated by Supercritical Carbon Dioxide and Conventional Solvent Evaporation Method. J Pharm Sci [Internet]. 2002 Sep 1;91(9):1948–57. Available from: http://linkinghub.elsevier.com/retrieve/pii/S0022354916310760

Crowley MM, Zhang F, Repka MA, Thumma S, Upadhye SB, Kumar Battu S, et al. Pharmaceutical Applications of Hot-Melt Extrusion: Part I. Drug Dev Ind Pharm [Internet]. 2007 Jan 26;33(9):909–26. Available from: http://www.ncbi.nlm.nih.gov/pubmed/17891577

Konno H, Handa T, Alonzo DE, Taylor LS. Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine. Eur J Pharm Biopharm [Internet]. 2008 Oct;70(2):493–9. Available from: http://www.ncbi.nlm.nih.gov/pubmed/18577451

Esfandyari-Manesh M, Mostafavi SH, Majidi RF, Koopaei MN, Ravari NS, Amini M, et al. Improved anticancer delivery of paclitaxel by albumin surface modification of PLGA nanoparticles. DARU J Pharm Sci [Internet]. 2015 Dec 23;23(1):28. Available from: http://www.darujps.com/content/23/1/28

Shah MK, Madan P, Lin S. Preparation, in vitro evaluation and statistical optimization of carvedilol-loaded solid lipid nanoparticles for lymphatic absorption via oral administration. Pharm Dev Technol [Internet]. 2014 Jun 23;19(4):475–85. Available from: http://www.tandfonline.com/doi/full/10.3109/10837450.2013.795169

Lin C-W, Cham T-M. Effect of particle size on the available surface area of nifedipine from nifedipine-polyethylene glycol 6000 solid dispersions. Int J Pharm [Internet]. 1996 Feb 17;127(2):261–72. Available from: http://www.sciencedirect.com/science/article/pii/0378517395042458

Baghel S, Cathcart H, O’Reilly NJ. Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs. J Pharm Sci [Internet]. 2016 Sep 1;105(9):2527–44. Available from: http://www.sciencedirect.com/science/article/pii/S002235491500009X

Kaushal AM, Chakraborti AK, Bansal AK. FTIR Studies on Differential Intermolecular Association in Crystalline and Amorphous States of Structurally Related Non-Steroidal Anti-Inflammatory Drugs. Mol Pharm [Internet]. 2008 Dec;5(6):937–45. Available from: http://pubs.acs.org/doi/abs/10.1021/mp800098d

Huang Y, Dai W-G. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharm Sin B [Internet]. 2014 Feb;4(1):18–25. Available from: http://linkinghub.elsevier.com/retrieve/pii/S2211383513000968

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