Exploring the effect of hydrophilic and hydrophobic structure of grafted polymeric micelles on drug loading

[Display omitted] 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...

Full description

Saved in:
Bibliographic Details
Published in:International journal of pharmaceutics 2016-10, Vol.512 (1), p.282-291
Main Authors: Shi, Chenjun, Sun, Yujiao, Wu, Haiyang, Zhu, Chengyun, Wei, Guoguang, Li, Jinfeng, Chan, Tenglan, Ouyang, Defang, Mao, Shirui
Format: Article
Language:English
Subjects:
Chitosan - chemistry
Drug Incompatibility
Drug-polymer compatibility
Flory-Huggins interaction parameter
Glycerides - chemistry
Grafted polymeric micelles
Hansen solubility parameter
Hydrophobic and Hydrophilic Interactions
Micelles
Models, Theoretical
Molecular Dynamics Simulation
Particle Size
Pharmaceutical Preparations - chemistry
Polymers - chemistry
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] 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 (χFH) and polarity difference (△Xp). 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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2016.08.054