Strategies for improving the payload of small molecular drugs in polymeric micelles

J Control Release. 2017 Sep 10:261:352-366. doi: 10.1016/j.jconrel.2017.01.047. Epub 2017 Feb 3.

Abstract

In the past few years, substantial efforts have been made in the design and preparation of polymeric micelles as novel drug delivery vehicles. Typically, polymeric micelles possess a spherical core-shell structure, with a hydrophobic core and a hydrophilic shell. Consequently, poorly water-soluble drugs can be effectively solubilized within the hydrophobic core, which can significantly boost their drug loading in aqueous media. This leads to new opportunities for some bioactive compounds that have previously been abandoned due to their low aqueous solubility. Even so, the payload of small molecular drugs is still not often satisfactory due to low drug loading and premature release, which makes it difficult to meet the requirements of in vivo studies. This problem has been a major focus in recent years. Following an analysis of the published literature in this field, several strategies towards achieving polymeric micelles with high drug loading and stability are presented in this review, in order to ensure adequate drug levels reach target sites.

Keywords: 10-Hydroxycamptothecin (PubChem CID: 97226); Amphotericin B (PubChem CID:5280965); Capecitabine (PubChem CID: 60953); Cisplatin (PubChem CID: 2767); Coenzyme Q10 (PubChem CID: 5281915); Docetaxel (PubChem CID: 148124); Doxorubicin (PubChem CID: 31703); Drug loading; Paclitaxel (PubChem CID: 36314); Payload; Polymeric micelles; Premature release; Small molecular drugs.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Carriers / chemistry*
  • Drug Delivery Systems*
  • Drug Liberation
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Micelles
  • Pharmaceutical Preparations / administration & dosage
  • Pharmaceutical Preparations / chemistry
  • Polymers / chemistry*
  • Solubility

Substances

  • Drug Carriers
  • Micelles
  • Pharmaceutical Preparations
  • Polymers