Colloidal nanostructured lipid carriers of pentoxifylline produced by microwave irradiation ameliorates imiquimod-induced psoriasis in mice

Vivek M. Ghate, Arun K. Kodoth, Abhishek Shah, Badalamoole Vishalakshi, Shaila A. Lewis

Research output: Contribution to journalArticle

Abstract

Psoriasis is a chronic inflammatory disease occurring due to a large cascade of molecular and biological processes. Pentoxifylline (PTX) has a profound anti-inflammatory activity and is clinically indicated in the management of psoriasis. PTX is highly hydrophilic and thus is permeation-limited to exert its action on the psoriatic lesions. Colloidal nanostructured lipid carriers (NLCs) is a boon for dermal drug delivery, but incorporation of hydrophilic medicaments is not only difficult to be achieved but is accompanied by suboptimal loading, erratic drug release and time-consuming. The present study was designed to develop NLCs incorporating PTX using the recently explored thin lipid film based microwave assisted rapid technique. Prior to the formulation, the crystal structure of PTX was analyzed by molecular modeling. NLCs formed within 4 min having a size of <200 nm, PDI of <0.250 and a surface charge <−28 mV. PTX was loaded and encapsulated to an extent of 10% and 90% in the NLCs. The drug flux was 4.848 μg/cm2/h at the end of 24 h with a detection of 14% in the receptor fluid indicating a higher retention of PTX within the skin (>84%). In addition, the PTX loaded NLCs were tested against imiquimod-induced psoriasis in mouse model. Histological examinations clearly showed a higher levels of remodeling of the skin layers compared to disease control. These results justify NLCs to be a promising topical delivery system for PTX during psoriasis and can be rapidly produced without the requirement of complex equipment and conditions.

Original languageEnglish
Pages (from-to)389-399
Number of pages11
JournalColloids and Surfaces B: Biointerfaces
Volume181
DOIs
Publication statusPublished - 01-09-2019

Fingerprint

imiquimod
Pentoxifylline
Microwave irradiation
Microwaves
Psoriasis
Lipids
mice
lipids
microwaves
irradiation
delivery
drugs
Disease control
Biological Phenomena
Skin
Molecular modeling
Drug delivery
Permeation
lesions
cascades

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Surfaces and Interfaces
  • Physical and Theoretical Chemistry
  • Colloid and Surface Chemistry

Cite this

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title = "Colloidal nanostructured lipid carriers of pentoxifylline produced by microwave irradiation ameliorates imiquimod-induced psoriasis in mice",
abstract = "Psoriasis is a chronic inflammatory disease occurring due to a large cascade of molecular and biological processes. Pentoxifylline (PTX) has a profound anti-inflammatory activity and is clinically indicated in the management of psoriasis. PTX is highly hydrophilic and thus is permeation-limited to exert its action on the psoriatic lesions. Colloidal nanostructured lipid carriers (NLCs) is a boon for dermal drug delivery, but incorporation of hydrophilic medicaments is not only difficult to be achieved but is accompanied by suboptimal loading, erratic drug release and time-consuming. The present study was designed to develop NLCs incorporating PTX using the recently explored thin lipid film based microwave assisted rapid technique. Prior to the formulation, the crystal structure of PTX was analyzed by molecular modeling. NLCs formed within 4 min having a size of <200 nm, PDI of <0.250 and a surface charge <−28 mV. PTX was loaded and encapsulated to an extent of 10{\%} and 90{\%} in the NLCs. The drug flux was 4.848 μg/cm2/h at the end of 24 h with a detection of 14{\%} in the receptor fluid indicating a higher retention of PTX within the skin (>84{\%}). In addition, the PTX loaded NLCs were tested against imiquimod-induced psoriasis in mouse model. Histological examinations clearly showed a higher levels of remodeling of the skin layers compared to disease control. These results justify NLCs to be a promising topical delivery system for PTX during psoriasis and can be rapidly produced without the requirement of complex equipment and conditions.",
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Colloidal nanostructured lipid carriers of pentoxifylline produced by microwave irradiation ameliorates imiquimod-induced psoriasis in mice. / Ghate, Vivek M.; Kodoth, Arun K.; Shah, Abhishek; Vishalakshi, Badalamoole; Lewis, Shaila A.

In: Colloids and Surfaces B: Biointerfaces, Vol. 181, 01.09.2019, p. 389-399.

Research output: Contribution to journalArticle

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