Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect

Yixian Li; Chung Kil Song; Min Kyoung Kim; Hyosang Lim; Qingbo Shen; Don Haeng Lee; Su Geun Yang

doi:10.1007/s12272-015-0604-9

Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect

Yixian Li, Chung Kil Song, Min Kyoung Kim, Hyosang Lim, Qingbo Shen, Don Haeng Lee, Su Geun Yang

Inha University

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

14 Scopus citations

Abstract

Megestrol acetate (MGA) belongs to the BCS class II drugs with low solubility and high permeability, and its oral absorption in conventional dosage form MGA microcrystal suspension (MGA MS) is very limited and greatly affected by food. In this study, MGA nanoemulsion (MGA NE) was formulated based on solubility, phase-diagram and release studies. Then oral bioavailability of MGA NE and MGA MS was evaluated. A randomized two-way crossover trial was conducted on six male dogs under fed and fasting conditions. Blood concentrations of MGA were analyzed using LC-MS/MS. MGA NE yielded 5.00-fold higher oral bioavailability in fasting conditions and displayed more stable absorption profiles after food intake compared with MGA MS.

Original language	English
Pages (from-to)	1850-1856
Number of pages	7
Journal	Archives of Pharmacal Research
Volume	38
Issue number	10
DOIs	https://doi.org/10.1007/s12272-015-0604-9
State	Published - 1 Oct 2015

Bibliographical note

Publisher Copyright:
© 2015 The Pharmaceutical Society of Korea.

Keywords

BCS class II drugs
Food-effect
Megestrol acetate
Nanoemulsion
Oral bioavailability

Access to Document

10.1007/s12272-015-0604-9

Cite this

@article{8b31e2676bb642c98c6a5998b0e0bb75,

title = "Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect",

abstract = "Megestrol acetate (MGA) belongs to the BCS class II drugs with low solubility and high permeability, and its oral absorption in conventional dosage form MGA microcrystal suspension (MGA MS) is very limited and greatly affected by food. In this study, MGA nanoemulsion (MGA NE) was formulated based on solubility, phase-diagram and release studies. Then oral bioavailability of MGA NE and MGA MS was evaluated. A randomized two-way crossover trial was conducted on six male dogs under fed and fasting conditions. Blood concentrations of MGA were analyzed using LC-MS/MS. MGA NE yielded 5.00-fold higher oral bioavailability in fasting conditions and displayed more stable absorption profiles after food intake compared with MGA MS.",

keywords = "BCS class II drugs, Food-effect, Megestrol acetate, Nanoemulsion, Oral bioavailability",

author = "Yixian Li and Song, \{Chung Kil\} and Kim, \{Min Kyoung\} and Hyosang Lim and Qingbo Shen and Lee, \{Don Haeng\} and Yang, \{Su Geun\}",

note = "Publisher Copyright: {\textcopyright} 2015 The Pharmaceutical Society of Korea.",

year = "2015",

month = oct,

day = "1",

doi = "10.1007/s12272-015-0604-9",

language = "English",

volume = "38",

pages = "1850--1856",

journal = "Archives of Pharmacal Research",

issn = "0253-6269",

publisher = "Pharmaceutical Society of Korea",

number = "10",

}

TY - JOUR

T1 - Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect

AU - Li, Yixian

AU - Song, Chung Kil

AU - Kim, Min Kyoung

AU - Lim, Hyosang

AU - Shen, Qingbo

AU - Lee, Don Haeng

AU - Yang, Su Geun

PY - 2015/10/1

Y1 - 2015/10/1

N2 - Megestrol acetate (MGA) belongs to the BCS class II drugs with low solubility and high permeability, and its oral absorption in conventional dosage form MGA microcrystal suspension (MGA MS) is very limited and greatly affected by food. In this study, MGA nanoemulsion (MGA NE) was formulated based on solubility, phase-diagram and release studies. Then oral bioavailability of MGA NE and MGA MS was evaluated. A randomized two-way crossover trial was conducted on six male dogs under fed and fasting conditions. Blood concentrations of MGA were analyzed using LC-MS/MS. MGA NE yielded 5.00-fold higher oral bioavailability in fasting conditions and displayed more stable absorption profiles after food intake compared with MGA MS.

AB - Megestrol acetate (MGA) belongs to the BCS class II drugs with low solubility and high permeability, and its oral absorption in conventional dosage form MGA microcrystal suspension (MGA MS) is very limited and greatly affected by food. In this study, MGA nanoemulsion (MGA NE) was formulated based on solubility, phase-diagram and release studies. Then oral bioavailability of MGA NE and MGA MS was evaluated. A randomized two-way crossover trial was conducted on six male dogs under fed and fasting conditions. Blood concentrations of MGA were analyzed using LC-MS/MS. MGA NE yielded 5.00-fold higher oral bioavailability in fasting conditions and displayed more stable absorption profiles after food intake compared with MGA MS.

KW - BCS class II drugs

KW - Food-effect

KW - Megestrol acetate

KW - Nanoemulsion

KW - Oral bioavailability

UR - https://www.scopus.com/pages/publications/84944145818

U2 - 10.1007/s12272-015-0604-9

DO - 10.1007/s12272-015-0604-9

M3 - Article

C2 - 25893430

AN - SCOPUS:84944145818

SN - 0253-6269

VL - 38

SP - 1850

EP - 1856

JO - Archives of Pharmacal Research

JF - Archives of Pharmacal Research

IS - 10

ER -

Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect

Abstract

Bibliographical note

Keywords

Access to Document

Other files and links

Fingerprint

Cite this