Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology
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Review Article Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology Athira R. Nair,1 Yarlagadda Dani Lakshman,1 Vullendula Sai Krishna Anand,1 K. S. Navya Sree,1 Krishnamurthy Bhat,1 and Swapnil J. Dengale1,2
Received 2 July 2020; accepted 7 October 2020 Abstract.
Solid dispersion is the preferred technology to prepare efficacious forms of BCS class-II/IV APIs. To prepare solid dispersions, there exist a wide variety of polymeric carriers with interesting physicochemical and thermochemical characteristics available at the disposal of a formulation scientist. Since the advent of the solid dispersion technology in the early 1960s, there have been more than 5000 scientific papers published in the subject area. This review discusses the polymeric carrier properties of most extensively used polymers PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus® in the solid dispersion technology. The literature trends about preparation techniques, dissolution, and stability improvement are analyzed from the Scopus® database to enable a formulator to make an informed choice of polymeric carrier. The stability and extent of dissolution improvement are largely dependent upon the type of polymeric carrier employed to formulate solid dispersions. With the increasing acceptance of transfer dissolution setup in the research community, it is required to evaluate the crystallization/precipitation inhibition potential of polymers under dynamic pH shift conditions. Further, there is a need to develop a regulatory framework which provides definition and complete classification along with necessarily recommended studies to characterize and evaluate solid dispersions.
KEYWORDS: solid dispersion; polymers; dissolution; solubility; stability.
INTRODUCTION In the quest to access the complex targets, most of the New Chemical Entities (NCEs) in the development pipeline are becoming increasingly lipophilic, thereby restricting their aqueous solubility. Therefore, a drug candidate with good permeability but limited aqueous solubility is not drug-like due to consequent lower bioavailability(1,2). For such candidates, which belong to Biopharmaceutical Classification class-II & IV (BCS-II & IV), improving the aqueous solubility is the most prudent option. To that end, various techniques have been employed to improve the solubility like micro/nanoparticle drug delivery (3), co-crystal formation (4,5), complexation with cyclodextrins (6,7), and salt formation (8). Nevertheless, success is usually marginal due to the inability of these techniques to
Supplementary Information The online version contains supplementary material available at https://doi.org/10.1208/s12249-020-01849-z. 1
Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, 576 104, India. 2 To whom correspondence should be addressed. (e–mail: [email protected])
generate and sustain the supersaturated state (9,10). In this regard, solid dispersion (SD) is considered as a promisi
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