Enhanced antimalarial activity of lumefantrine nanopowder prepared by wet-milling DYNO MILL technique

Sachin Gahoi; Gaurav K. Jain; Renu Tripathi; Swaroop K. Pandey; Mohammed Anwar; Musarrat H. Warsi; Mayank Singhal; Roop K. Khar; Farhan J. Ahmad

doi:10.1016/j.colsurfb.2012.01.047

Enhanced antimalarial activity of lumefantrine nanopowder prepared by wet-milling DYNO MILL technique

Sachin Gahoi, Gaurav K. Jain, Renu Tripathi, Swaroop K. Pandey, Mohammed Anwar, Musarrat H. Warsi, Mayank Singhal, Roop K. Khar, Farhan J. Ahmad

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

36 Scopus citations

Abstract

Lumefantrine (LMF) is an antimalarial drug that exhibits poor oral bioavailability, owing to its poor aqueous solubility. To improve its antimalarial activity, nanopowder formulation using DYNO MILL was prepared. Combination of HPMC E3 (4%, w/v) and Tween 80 (2.5%, w/v) as dispersing agents, favored the production of smaller LMF particles with mean size of 0.251μm. LMF nanopowder showed enhanced dissolution rate attributed to nanonization of LMF. The IC ₅₀ value of nano-sized LMF was found to be 0.1ng/mL, which was 175-times lower than the IC ₅₀ value of unmilled LMF powder (17.5ng/mL) and 42-times lower than the IC ₅₀ value of chloroquine (4.2ng/mL). The in vivo antimalarial activity demonstrated an enhanced antimalarial potential of LMF nanopowder against P. Yoelii nigeriensis compared to unmilled drug. Wet-milling using DYNO MILL offers a highly effective approach to produce stable drug nanopowders. Furthermore, LMF nanopowder makes the Coartem ^® therapy more effective.

Original language	English
Pages (from-to)	16-22
Number of pages	7
Journal	Colloids and Surfaces B: Biointerfaces
Volume	95
DOIs	https://doi.org/10.1016/j.colsurfb.2012.01.047
State	Published - 15 Jun 2012
Externally published	Yes

Keywords

Antimalarial
Dissolution rate
Lumefantrine
Nanopowder
Wet-milling

ASJC Scopus subject areas

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

UN SDGs

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

Access to Document

10.1016/j.colsurfb.2012.01.047

Cite this

@article{77db6beeefa743108291a4bb801c38af,

title = "Enhanced antimalarial activity of lumefantrine nanopowder prepared by wet-milling DYNO MILL technique",

abstract = "Lumefantrine (LMF) is an antimalarial drug that exhibits poor oral bioavailability, owing to its poor aqueous solubility. To improve its antimalarial activity, nanopowder formulation using DYNO MILL was prepared. Combination of HPMC E3 (4%, w/v) and Tween 80 (2.5%, w/v) as dispersing agents, favored the production of smaller LMF particles with mean size of 0.251μm. LMF nanopowder showed enhanced dissolution rate attributed to nanonization of LMF. The IC 50 value of nano-sized LMF was found to be 0.1ng/mL, which was 175-times lower than the IC 50 value of unmilled LMF powder (17.5ng/mL) and 42-times lower than the IC 50 value of chloroquine (4.2ng/mL). The in vivo antimalarial activity demonstrated an enhanced antimalarial potential of LMF nanopowder against P. Yoelii nigeriensis compared to unmilled drug. Wet-milling using DYNO MILL offers a highly effective approach to produce stable drug nanopowders. Furthermore, LMF nanopowder makes the Coartem {\textregistered} therapy more effective.",

keywords = "Antimalarial, Dissolution rate, Lumefantrine, Nanopowder, Wet-milling",

author = "Sachin Gahoi and Jain, {Gaurav K.} and Renu Tripathi and Pandey, {Swaroop K.} and Mohammed Anwar and Warsi, {Musarrat H.} and Mayank Singhal and Khar, {Roop K.} and Ahmad, {Farhan J.}",

year = "2012",

month = jun,

day = "15",

doi = "10.1016/j.colsurfb.2012.01.047",

language = "English",

volume = "95",

pages = "16--22",

journal = "Colloids and Surfaces B: Biointerfaces",

issn = "0927-7765",

publisher = "Elsevier B.V.",

}

TY - JOUR

T1 - Enhanced antimalarial activity of lumefantrine nanopowder prepared by wet-milling DYNO MILL technique

AU - Gahoi, Sachin

AU - Jain, Gaurav K.

AU - Tripathi, Renu

AU - Pandey, Swaroop K.

AU - Anwar, Mohammed

AU - Warsi, Musarrat H.

AU - Singhal, Mayank

AU - Khar, Roop K.

AU - Ahmad, Farhan J.

PY - 2012/6/15

Y1 - 2012/6/15

N2 - Lumefantrine (LMF) is an antimalarial drug that exhibits poor oral bioavailability, owing to its poor aqueous solubility. To improve its antimalarial activity, nanopowder formulation using DYNO MILL was prepared. Combination of HPMC E3 (4%, w/v) and Tween 80 (2.5%, w/v) as dispersing agents, favored the production of smaller LMF particles with mean size of 0.251μm. LMF nanopowder showed enhanced dissolution rate attributed to nanonization of LMF. The IC 50 value of nano-sized LMF was found to be 0.1ng/mL, which was 175-times lower than the IC 50 value of unmilled LMF powder (17.5ng/mL) and 42-times lower than the IC 50 value of chloroquine (4.2ng/mL). The in vivo antimalarial activity demonstrated an enhanced antimalarial potential of LMF nanopowder against P. Yoelii nigeriensis compared to unmilled drug. Wet-milling using DYNO MILL offers a highly effective approach to produce stable drug nanopowders. Furthermore, LMF nanopowder makes the Coartem ® therapy more effective.

AB - Lumefantrine (LMF) is an antimalarial drug that exhibits poor oral bioavailability, owing to its poor aqueous solubility. To improve its antimalarial activity, nanopowder formulation using DYNO MILL was prepared. Combination of HPMC E3 (4%, w/v) and Tween 80 (2.5%, w/v) as dispersing agents, favored the production of smaller LMF particles with mean size of 0.251μm. LMF nanopowder showed enhanced dissolution rate attributed to nanonization of LMF. The IC 50 value of nano-sized LMF was found to be 0.1ng/mL, which was 175-times lower than the IC 50 value of unmilled LMF powder (17.5ng/mL) and 42-times lower than the IC 50 value of chloroquine (4.2ng/mL). The in vivo antimalarial activity demonstrated an enhanced antimalarial potential of LMF nanopowder against P. Yoelii nigeriensis compared to unmilled drug. Wet-milling using DYNO MILL offers a highly effective approach to produce stable drug nanopowders. Furthermore, LMF nanopowder makes the Coartem ® therapy more effective.

KW - Antimalarial

KW - Dissolution rate

KW - Lumefantrine

KW - Nanopowder

KW - Wet-milling

UR - http://www.scopus.com/inward/record.url?scp=84860549641&partnerID=8YFLogxK

U2 - 10.1016/j.colsurfb.2012.01.047

DO - 10.1016/j.colsurfb.2012.01.047

M3 - Article

C2 - 22439975

AN - SCOPUS:84860549641

SN - 0927-7765

VL - 95

SP - 16

EP - 22

JO - Colloids and Surfaces B: Biointerfaces

JF - Colloids and Surfaces B: Biointerfaces

ER -

Enhanced antimalarial activity of lumefantrine nanopowder prepared by wet-milling DYNO MILL technique

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this