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Pharmaceutics
Special Issues
Micellar Drug Delivery
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Micellar Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (30 November 2012) | Viewed by 32055

Special Issue Editor

Prof. Dr. Vladimir P. Torchilin

E-Mail Website
Guest Editor
University Distinguished Professor, Director, Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, 140 The Fenway, room 214, 360 Huntington Avenue Boston, MA 02115, USA
Interests: drug carriers; drug delivery sytems; drug targeting; liposomes; micelles; experimental cancer immunology; imaging agents
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Micells including polymeric micelles represent an important class of pharmaceutical carriers for poorly soluble diagnostic and therapeutic agents. Sable micelles with low CMC values maintain stability upon dilution and in biological fluids, demonstrate prolonged circulation times in vivo, and can be effectively loaded with various poorly soluble pharmaceuticals. Drug-loaded micelles demonstrate an increased accumulation in tumors via the enhanced permeability and retention (EPR) effect, and cytotoxicity of micellar formulations is usually markedly higher compared to free drugs. The potential of micellar drugs may be further improved by attaching targeting ligands, such as specific antibodies, to the micelle surface. By proper modification or synthetic chemistry, the micelles could be made stimuli-sensitive and capable of intracellular penetration. Many of these aspects of micellar drug delivery systems will be considered in this issue.

Prof. Dr. Vladimir P. Torchilin
Guest Editor

Keywords

  • pharmaceutical micelles
  • polymeric micelles
  • lipid-core micelles
  • drug delivery
  • drug targeting
  • poorly soluble drugs
  • drug solubilization

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Published Papers (3 papers)

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13 pages, 470 KiB  
Article
Pharmacokinetic Evaluation of a DSPE-PEG2000 Micellar Formulation of Ridaforolimus in Rat
by Connie M. Remsberg, Yunqi Zhao, Jody K. Takemoto, Rebecca M. Bertram, Neal M. Davies and Marcus Laird Forrest
Pharmaceutics 2013, 5(1), 81-93; https://doi.org/10.3390/pharmaceutics5010081 - 27 Dec 2012
Cited by 14 | Viewed by 9072
Abstract
The rapamycin analog, ridaforolimus, has demonstrated potent anti-proliferative effects in cancer treatment, and it currently is being evaluated in a range of clinical cancer studies. Ridaforolimus is an extremely lipophilic compound with limited aqueous solubility, which may benefit from formulation with polymeric micelles. [...] Read more.
The rapamycin analog, ridaforolimus, has demonstrated potent anti-proliferative effects in cancer treatment, and it currently is being evaluated in a range of clinical cancer studies. Ridaforolimus is an extremely lipophilic compound with limited aqueous solubility, which may benefit from formulation with polymeric micelles. Herein, we report the encapsulation of ridaforolimus in 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000) (DSPE-PEG2000) via a solvent extraction technique. Micelle loading greatly improved the solubility of ridaforolimus by approximately 40 times from 200 μg/mL to 8.9 mg/mL. The diameters of the drug-loaded micelles were 33 ± 15 nm indicating they are of appropriate size to accumulate within the tumor site via the enhanced permeability and retention (EPR) effect. The DSPE-PEG2000 micelle formulation was dosed intravenously to rats at 10 mg/kg and compared to a control of ridaforolimus in ethanol/PEG 400. The micelle significantly increased the half-life of ridaforolimus by 170% and decreased the clearance by 58%, which is consistent with improved retention of the drug in the plasma by the micelle formulation. Full article
(This article belongs to the Special Issue Micellar Drug Delivery)
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Review

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24 pages, 345 KiB  
Review
Polysaccharide-Based Micelles for Drug Delivery
by Nan Zhang, Patricia R. Wardwell and Rebecca A. Bader
Pharmaceutics 2013, 5(2), 329-352; https://doi.org/10.3390/pharmaceutics5020329 - 27 May 2013
Cited by 202 | Viewed by 13678
Abstract
Delivery of hydrophobic molecules and proteins has been an issue due to poor bioavailability following administration. Thus, micelle carrier systems are being investigated to improve drug solubility and stability. Due to problems with toxicity and immunogenicity, natural polysaccharides are being explored as substitutes [...] Read more.
Delivery of hydrophobic molecules and proteins has been an issue due to poor bioavailability following administration. Thus, micelle carrier systems are being investigated to improve drug solubility and stability. Due to problems with toxicity and immunogenicity, natural polysaccharides are being explored as substitutes for synthetic polymers in the development of new micelle systems. By grafting hydrophobic moieties to the polysaccharide backbone, self-assembled micelles can be readily formed in aqueous solution. Many polysaccharides also possess inherent bioactivity that can facilitate mucoadhesion, enhanced targeting of specific tissues, and a reduction in the inflammatory response. Furthermore, the hydrophilic nature of some polysaccharides can be exploited to enhance circulatory stability. This review will highlight the advantages of polysaccharide use in the development of drug delivery systems and will provide an overview of the polysaccharide-based micelles that have been developed to date. Full article
(This article belongs to the Special Issue Micellar Drug Delivery)
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19 pages, 269 KiB  
Review
Exploring Polymeric Micelles for Improved Delivery of Anticancer Agents: Recent Developments in Preclinical Studies
by Chalet Tan, Yingzhe Wang and Wei Fan
Pharmaceutics 2013, 5(1), 201-219; https://doi.org/10.3390/pharmaceutics5010201 - 22 Mar 2013
Cited by 61 | Viewed by 8427
Abstract
As versatile drug delivery systems, polymeric micelles have demonstrated particular strength in solubilizing hydrophobic anticancer drugs while eliminating the use of toxic organic solvents and surfactants. However, the true promise of polymeric micelles as drug carriers for cancer therapy resides in their potential [...] Read more.
As versatile drug delivery systems, polymeric micelles have demonstrated particular strength in solubilizing hydrophobic anticancer drugs while eliminating the use of toxic organic solvents and surfactants. However, the true promise of polymeric micelles as drug carriers for cancer therapy resides in their potential ability to preferentially elevate drug exposure in the tumor and achieve enhanced anticancer efficacy, which still remains to be fully exploited. Here, we review various micellar constructs that exhibit the enhanced permeation and retention effect in the tumor, the targeting ligands that potentiate the anticancer efficacy of micellar drugs, and the polyplex micelle systems suitable for the delivery of plasmid DNA and small interference RNA. Together, these preclinical studies in animal models help us further explore polymeric micelles as emerging drug carriers for targeted cancer therapy. Full article
(This article belongs to the Special Issue Micellar Drug Delivery)
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