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Exploring the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading
Shi C.1; Sun Y.1; Wu H.1; Zhu C.1; Wei G.1; Li J.1; Chan T.2; Ouyang D.2; Mao S.1
2016-10-15
Source PublicationInternational Journal of Pharmaceutics
ISSN18733476 03785173
Volume512Issue:1Pages:282-291
Abstract

The objective of this paper is to explore the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading, and elucidate whether drug-polymer compatibility, as predicted by Hansen solubility parameters (HSPs), can be used as a tool for drug-polymer pairs screening and guide the design of grafted polymeric micelles. HSPs of 27 drugs and three grafted copolymers were calculated according to group contribution method. The drug-polymer compatibilities were evaluated using the approaches of Flory-Huggins interaction parameters (χ) and polarity difference (△X). Two models, model A and B, were put forward for drug-polymer compatibility prediction. In model A, hydrophilic/hydrophobic part as a whole was regarded as one segment. And, in model B, hydrophilic and hydrophobic segments were evaluated individually. First of all, using chitosan (CS)-grafted-glyceryl monooeate (GMO) based micelle as an example, the suitability of model A and model B for predicating drug-polymer compatibility was evaluated theoretically. Thereafter, corresponding experiments were carried out to check the validity of the theoretical prediction. It was demonstrated that Model B, which evaluates drug compatibility with both hydrophilic and hydrophobic segments of the copolymer, is more reliable for drug-polymer compatibility prediction. Moreover, the approach of model B allows for the selection of a defined grafted polymer with for a specific drug and vice versa. Thus, drug compatibility evaluation via HSPs with both hydrophilic and hydrophobic segments is a suitable tool for the rational design of grafted polymeric micelles. The molecular dynamics (MD) simulation study provided further support to the established model and experimental results.

KeywordDrug-polymer Compatibility Flory-huggins Interaction Parameter Grafted Polymeric Micelles Hansen Solubility Parameter
DOI10.1016/j.ijpharm.2016.08.054
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000384863700030
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Cited Times [WOS]:7   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Shenyang Pharmaceutical University
2.Universidade de Macau
Recommended Citation
GB/T 7714
Shi C.,Sun Y.,Wu H.,et al. Exploring the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading[J]. International Journal of Pharmaceutics,2016,512(1):282-291.
APA Shi C..,Sun Y..,Wu H..,Zhu C..,Wei G..,...&Mao S..(2016).Exploring the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading.International Journal of Pharmaceutics,512(1),282-291.
MLA Shi C.,et al."Exploring the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading".International Journal of Pharmaceutics 512.1(2016):282-291.
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