Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method

Lesego Tshweu; Lebogang Katata; Lonji Kalombo; Diego A. Chiappetta; Christian Hocht; Alejandro Sosnik; Hulda Swai

doi:10.2217/NNM.13.167

Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method

Lesego Tshweu, Lebogang Katata, Lonji Kalombo, Diego A. Chiappetta, Christian Hocht, Alejandro Sosnik, Hulda Swai

Materials Science & Engineering

Technion - Israel Institute of Technology

Research output: Contribution to journal › Article › peer-review

Abstract

Aim: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. Materials & methods: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. Results: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. Conclusion: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.

Original language	English
Pages (from-to)	1821-1833
Number of pages	13
Journal	Nanomedicine
Volume	9
Issue number	12
DOIs	https://doi.org/10.2217/NNM.13.167
State	Published - 1 Aug 2014

Keywords

Efavirenz •
Hiv •
In vitro drug release •
Oral bioavailability enhancement •
Poly(epsilon-caprolactone) nanoparticle •
Spray drying

All Science Journal Classification (ASJC) codes

Bioengineering
Medicine (miscellaneous)
Biomedical Engineering
General Materials Science

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.2217/NNM.13.167

Cite this

@article{28aec1b60f4a442598815a2908a92444,

title = "Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method",

abstract = "Aim: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. Materials & methods: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. Results: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. Conclusion: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.",

keywords = "Efavirenz •, Hiv •, In vitro drug release •, Oral bioavailability enhancement •, Poly(epsilon-caprolactone) nanoparticle •, Spray drying",

author = "Lesego Tshweu and Lebogang Katata and Lonji Kalombo and Chiappetta, {Diego A.} and Christian Hocht and Alejandro Sosnik and Hulda Swai",

note = "Publisher Copyright: {\textcopyright} 2014 Future Medicine Ltd.",

year = "2014",

month = aug,

day = "1",

doi = "10.2217/NNM.13.167",

language = "الإنجليزيّة",

volume = "9",

pages = "1821--1833",

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TY - JOUR

T1 - Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method

AU - Tshweu, Lesego

AU - Katata, Lebogang

AU - Kalombo, Lonji

AU - Chiappetta, Diego A.

AU - Hocht, Christian

AU - Sosnik, Alejandro

AU - Swai, Hulda

PY - 2014/8/1

Y1 - 2014/8/1

N2 - Aim: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. Materials & methods: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. Results: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. Conclusion: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.

AB - Aim: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. Materials & methods: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. Results: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. Conclusion: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.

KW - Efavirenz •

KW - Hiv •

KW - In vitro drug release •

KW - Oral bioavailability enhancement •

KW - Poly(epsilon-caprolactone) nanoparticle •

KW - Spray drying

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U2 - 10.2217/NNM.13.167

DO - 10.2217/NNM.13.167

M3 - مقالة

C2 - 24364871

SN - 1743-5889

VL - 9

SP - 1821

EP - 1833

JO - Nanomedicine

JF - Nanomedicine

IS - 12

ER -

Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method

Abstract

Keywords

All Science Journal Classification (ASJC) codes

UN SDGs

Access to Document

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