Polyglycolized saturated glyceride as a carrier and enhancer for drug penetration

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

In this study, the influence of the melting point and HLB (hydrophile-lipophile balance) value of Gelucire® -based formulations on the permeation of model drugs, including prostaglandin E1 (PGE1) and its alkyl esters, through the skin barrier was examined. Seven formulations consisting of three grades of Gelucire (44/14, 50/02, and 37/02) at different ratios with the addition of lauroglycol at a fixed ratio of 4: 1 to a total Gelucire amount were prepared with model drugs at a concentration of 0.1 mg/mg. For (PGE1), the maximal flux at this concentration was about 35.95 nmole/cm2 per h and occurred at the HLB value of 6.6; the melting point ranged from 49 to 54 °C. For the methyl ester of PGE1, the maximal flux appeared to be 76.62 nmole/cm2 per h and occurred at the HLB value of 5.3; the melting point ranged from 46 to 50 °C. For the ethyl ester of PGE1, the maximal flux was around 33.45 nmole/cm2 per h and occurred at the HLB value of 5.3; the melting point ranged from 46 to 50 °C. The maximal flux was 15.46 nmol/cm2 per h for the isopropyl ester of PGE1 and appeared at the HLB of 5.3; the melting point ranged from 46 to 50 °C. The maximal flux of the butyl ester of PGE1 was around 13.67 nmol/cm2 per h and occurred at the HLB value of 6.6; the melting point ranged from 41 to 48 °C. The promotion of penetration for PGE1 and its alkyl esters seemed to be maximized with different Gelucire systems. Results also demonstrate that a higher melting point and a lower HLB value of Gelucire 50/02 resulted in a decreased permeation rate of PGE1 alkyl esters. But the tendency for Gelucire 50/02 and 37/02 to promote the penetration of PGE1 alkyl esters was similar, and the extent of the influence decreased with increased alkyl chain length. This is possibly explained by the fact that Gelucire 50/02 and 37/02 have the same HLB value. Similarly, the influence on drug flux of the HLB value of the Gelucire system was more profound than that of the melting point in this study.

Original languageEnglish
Pages (from-to)107-118
Number of pages12
JournalChinese Pharmaceutical Journal
Volume53
Issue number3
Publication statusPublished - 2001

Fingerprint

Glycerides
Drug Carriers
Alprostadil
Freezing
Melting point
Esters
Fluxes
Pharmaceutical Preparations
Permeation
Chain length
Skin

Keywords

  • Alkyl ester
  • Gelucire®
  • Penetration
  • Prostaglandin E

ASJC Scopus subject areas

  • Bioengineering
  • Pharmaceutical Science

Cite this

Polyglycolized saturated glyceride as a carrier and enhancer for drug penetration. / Sheu, M. T.; Hsia, A.; Ho, H. O.

In: Chinese Pharmaceutical Journal, Vol. 53, No. 3, 2001, p. 107-118.

Research output: Contribution to journalArticle

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N2 - In this study, the influence of the melting point and HLB (hydrophile-lipophile balance) value of Gelucire® -based formulations on the permeation of model drugs, including prostaglandin E1 (PGE1) and its alkyl esters, through the skin barrier was examined. Seven formulations consisting of three grades of Gelucire (44/14, 50/02, and 37/02) at different ratios with the addition of lauroglycol at a fixed ratio of 4: 1 to a total Gelucire amount were prepared with model drugs at a concentration of 0.1 mg/mg. For (PGE1), the maximal flux at this concentration was about 35.95 nmole/cm2 per h and occurred at the HLB value of 6.6; the melting point ranged from 49 to 54 °C. For the methyl ester of PGE1, the maximal flux appeared to be 76.62 nmole/cm2 per h and occurred at the HLB value of 5.3; the melting point ranged from 46 to 50 °C. For the ethyl ester of PGE1, the maximal flux was around 33.45 nmole/cm2 per h and occurred at the HLB value of 5.3; the melting point ranged from 46 to 50 °C. The maximal flux was 15.46 nmol/cm2 per h for the isopropyl ester of PGE1 and appeared at the HLB of 5.3; the melting point ranged from 46 to 50 °C. The maximal flux of the butyl ester of PGE1 was around 13.67 nmol/cm2 per h and occurred at the HLB value of 6.6; the melting point ranged from 41 to 48 °C. The promotion of penetration for PGE1 and its alkyl esters seemed to be maximized with different Gelucire systems. Results also demonstrate that a higher melting point and a lower HLB value of Gelucire 50/02 resulted in a decreased permeation rate of PGE1 alkyl esters. But the tendency for Gelucire 50/02 and 37/02 to promote the penetration of PGE1 alkyl esters was similar, and the extent of the influence decreased with increased alkyl chain length. This is possibly explained by the fact that Gelucire 50/02 and 37/02 have the same HLB value. Similarly, the influence on drug flux of the HLB value of the Gelucire system was more profound than that of the melting point in this study.

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