Inclusion of digestible surfactants in solid SMEDDS formulation removes lag time and influences the formation of structured particles during digestion

Kapilkumar Vithani, Adrian Hawley, Vincent Jannin, Colin Pouton, Ben J Boyd

Research output: Contribution to journalArticleResearchpeer-review

Abstract

Solid self-microemulsifying drug delivery systems (SMEDDS) have received considerable attention in recent times attempting to overcome the drawbacks of liquid SMEDDS. Earlier literature reports on solid SMEDDS have focussed on formulation development; however, the digestibility and propensity for self-assembly of the digested components with endogenous bile salts and phospholipids are unknown. Therefore, as a starting point, previously reported solid SMEDDS containing Gelucire® 44/14 (GEL) and the non-digestible surfactants, Vitamin E TPGS (TPGS) and Lutrol® F 127 (F 127), were prepared, and their dispersion and digestion behaviours were studied using an in vitro lipolysis model, coupled with small-angle X-ray scattering (SAXS) to determine the formed colloidal structures during digestion in real time. GEL alone was digested (89%) and formed a lamellar phase (Lα). When surfactants were added at a 40:60% w/w lipid to surfactants ratio, digestion was inhibited with a significant lag time being evident. However, increasing the fraction of GEL to 50% w/w enabled digestion with reduced lag time. The substitution of the non-digestible surfactants with digestible surfactants, sucrose esters S-1670 (S-1670) and Span® 60 (S-60), eliminated the digestion lag time, and the formation of colloidal structures was more similar to that of GEL alone.

Original languageEnglish
Pages (from-to)754-764
Number of pages11
JournalThe AAPS Journal
Volume19
Issue number3
DOIs
Publication statusPublished - 1 May 2017

Cite this

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title = "Inclusion of digestible surfactants in solid SMEDDS formulation removes lag time and influences the formation of structured particles during digestion",
abstract = "Solid self-microemulsifying drug delivery systems (SMEDDS) have received considerable attention in recent times attempting to overcome the drawbacks of liquid SMEDDS. Earlier literature reports on solid SMEDDS have focussed on formulation development; however, the digestibility and propensity for self-assembly of the digested components with endogenous bile salts and phospholipids are unknown. Therefore, as a starting point, previously reported solid SMEDDS containing Gelucire{\circledR} 44/14 (GEL) and the non-digestible surfactants, Vitamin E TPGS (TPGS) and Lutrol{\circledR} F 127 (F 127), were prepared, and their dispersion and digestion behaviours were studied using an in vitro lipolysis model, coupled with small-angle X-ray scattering (SAXS) to determine the formed colloidal structures during digestion in real time. GEL alone was digested (89{\%}) and formed a lamellar phase (Lα). When surfactants were added at a 40:60{\%} w/w lipid to surfactants ratio, digestion was inhibited with a significant lag time being evident. However, increasing the fraction of GEL to 50{\%} w/w enabled digestion with reduced lag time. The substitution of the non-digestible surfactants with digestible surfactants, sucrose esters S-1670 (S-1670) and Span{\circledR} 60 (S-60), eliminated the digestion lag time, and the formation of colloidal structures was more similar to that of GEL alone.",
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Inclusion of digestible surfactants in solid SMEDDS formulation removes lag time and influences the formation of structured particles during digestion. / Vithani, Kapilkumar; Hawley, Adrian; Jannin, Vincent; Pouton, Colin; Boyd, Ben J.

In: The AAPS Journal, Vol. 19, No. 3, 01.05.2017, p. 754-764.

Research output: Contribution to journalArticleResearchpeer-review

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