Inclusion of Digestible Surfactants in Solid SMEDDS Formulation Removes Lag Time and Influences the Formation of Structured Particles During Digestion.
Identifieur interne : 000998 ( PubMed/Checkpoint ); précédent : 000997; suivant : 000999Inclusion of Digestible Surfactants in Solid SMEDDS Formulation Removes Lag Time and Influences the Formation of Structured Particles During Digestion.
Auteurs : Kapilkumar Vithani [Australie] ; Adrian Hawley [Australie] ; Vincent Jannin [France] ; Colin Pouton [Australie] ; Ben J. Boyd [Australie]Source :
- The AAPS journal [ 1550-7416 ] ; 2017.
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.
DOI: 10.1208/s12248-016-0036-6
PubMed: 28116678
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Boyd</name><affiliation wicri:level="1"><nlm:affiliation>Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Parkville, Victoria, 3052, Australia. ben.boyd@monash.edu.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Parkville, Victoria, 3052</wicri:regionArea><wicri:noRegion>3052</wicri:noRegion></affiliation></author></analytic><series><title level="j">The AAPS journal</title><idno type="eISSN">1550-7416</idno><imprint><date when="2017" type="published">2017</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">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.</div></front></TEI><pubmed><MedlineCitation Status="In-Process" Owner="NLM"><PMID Version="1">28116678</PMID><DateCreated><Year>2017</Year><Month>01</Month><Day>24</Day></DateCreated><DateRevised><Year>2017</Year><Month>11</Month><Day>09</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1550-7416</ISSN><JournalIssue CitedMedium="Internet"><Volume>19</Volume><Issue>3</Issue><PubDate><Year>2017</Year><Month>May</Month></PubDate></JournalIssue><Title>The AAPS journal</Title><ISOAbbreviation>AAPS J</ISOAbbreviation></Journal><ArticleTitle>Inclusion of Digestible Surfactants in Solid SMEDDS Formulation Removes Lag Time and Influences the Formation of Structured Particles During Digestion.</ArticleTitle><Pagination><MedlinePgn>754-764</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1208/s12248-016-0036-6</ELocationID><Abstract><AbstractText>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.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Vithani</LastName><ForeName>Kapilkumar</ForeName><Initials>K</Initials><AffiliationInfo><Affiliation>Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Parkville, Victoria, 3052, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Hawley</LastName><ForeName>Adrian</ForeName><Initials>A</Initials><AffiliationInfo><Affiliation>SAXS/WAXS Beamtime, Australian Synchrotron, Clayton, Victoria, 3168, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Jannin</LastName><ForeName>Vincent</ForeName><Initials>V</Initials><AffiliationInfo><Affiliation>Gattefossé SAS, 36 Chemin de Genas, 69804, Saint-Priest, France.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Pouton</LastName><ForeName>Colin</ForeName><Initials>C</Initials><AffiliationInfo><Affiliation>Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Parkville, Victoria, 3052, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Boyd</LastName><ForeName>Ben J</ForeName><Initials>BJ</Initials><AffiliationInfo><Affiliation>Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Parkville, Victoria, 3052, Australia. ben.boyd@monash.edu.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash University (Parkville Campus), Parkville, Victoria, 3052, Australia. ben.boyd@monash.edu.</Affiliation></AffiliationInfo></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2017</Year><Month>01</Month><Day>23</Day></ArticleDate></Article><MedlineJournalInfo><Country>United States</Country><MedlineTA>AAPS J</MedlineTA><NlmUniqueID>101223209</NlmUniqueID><ISSNLinking>1550-7416</ISSNLinking></MedlineJournalInfo><CommentsCorrectionsList><CommentsCorrections RefType="Cites"><RefSource>Pharm Res. 2004 Feb;21(2):254-60</RefSource><PMID Version="1">15032306</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>Pharm Res. 1990 Jul;7(7):756-61</RefSource><PMID Version="1">2395805</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>Int J Pharm. 2004 Mar 19;272(1-2):1-10</RefSource><PMID 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Jun;33(19):4889-906</RefSource><PMID Version="1">22498300</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>J Pharm Sci. 2005 Mar;94(3):481-92</RefSource><PMID Version="1">15619248</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>Colloids Surf B Biointerfaces. 2013 Dec 1;112:337-43</RefSource><PMID Version="1">24012665</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>J Pharm Pharmacol. 2002 Jan;54(1):29-41</RefSource><PMID Version="1">11833493</PMID></CommentsCorrections></CommentsCorrectionsList><KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="N">in vitro lipolysis</Keyword><Keyword MajorTopicYN="N">lipid digestion</Keyword><Keyword MajorTopicYN="N">non-digestible and digestible surfactants</Keyword><Keyword MajorTopicYN="N">small-angle X-ray scattering</Keyword><Keyword MajorTopicYN="N">solid SMEDDS</Keyword></KeywordList></MedlineCitation><PubmedData><History><PubMedPubDate 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Kapilkumar" sort="Vithani, Kapilkumar" uniqKey="Vithani K" first="Kapilkumar" last="Vithani">Kapilkumar Vithani</name></noRegion><name sortKey="Boyd, Ben J" sort="Boyd, Ben J" uniqKey="Boyd B" first="Ben J" last="Boyd">Ben J. 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