A Novel Semi-Solid Self-Emulsifying Formulation of Aprepitant for Oral Delivery: An In Vitro Evaluation

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dc.authoridAkbal-Dagistan, Ozlem/0000-0002-6524-3535
dc.authoridOZSOY, YILDIZ/0000-0002-9110-3704
dc.authorwosidAkbal-Dagistan, Ozlem/Q-1443-2019
dc.contributor.authorNazli, Hakan
dc.contributor.authorMesut, Burcu
dc.contributor.authorAkbal-Dagistan, Ozlem
dc.contributor.authorOzsoy, Yildiz
dc.date.accessioned2024-06-12T11:15:49Z
dc.date.available2024-06-12T11:15:49Z
dc.date.issued2023
dc.departmentTrakya Üniversitesien_US
dc.description.abstractAprepitant is the first member of a relatively new antiemetic drug class called NK1 receptor antagonists. It is commonly prescribed to prevent chemotherapy-induced nausea and vomiting. Although it is included in many treatment guidelines, its poor solubility causes bioavailability issues. A particle size reduction technique was used in the commercial formulation to overcome low bioavailability. Production with this method consists of many successive steps that cause the cost of the drug to increase. This study aims to develop an alternative, cost-effective formulation to the existing nanocrystal form. We designed a self-emulsifying formulation that can be filled into capsules in a melted state and then solidified at room temperature. Solidification was achieved by using surfactants with a melting temperature above room temperature. Various polymers have also been tested to maintain the supersaturated state of the drug. The optimized formulation consists of CapryolTM 90, Kolliphor((R)) CS20, Transcutol((R)) P, and Soluplus((R)); it was characterized by DLS, FTIR, DSC, and XRPD techniques. A lipolysis test was conducted to predict the digestion performance of formulations in the gastrointestinal system. Dissolution studies showed an increased dissolution rate of the drug. Finally, the cytotoxicity of the formulation was tested in the Caco-2 cell line. According to the results, a formulation with improved solubility and low toxicity was obtained.en_US
dc.description.sponsorshipIstanbul University [29467]en_US
dc.description.sponsorshipThis research was funded by Istanbul University Scientific Research Projects Unit, grant number 29467. The APC was also funded by Istanbul University.en_US
dc.identifier.doi10.3390/pharmaceutics15051509
dc.identifier.issn1999-4923
dc.identifier.issue5en_US
dc.identifier.pmid37242751en_US
dc.identifier.scopus2-s2.0-85160439296en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.3390/pharmaceutics15051509
dc.identifier.urihttps://hdl.handle.net/20.500.14551/24088
dc.identifier.volume15en_US
dc.identifier.wosWOS:000997201600001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherMdpien_US
dc.relation.ispartofPharmaceuticsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectSupersaturated SNEDDSen_US
dc.subjectCapsule Filled SNEDDSen_US
dc.subjectSemi-Solid SNEDDSen_US
dc.subjectSolubility Enhancementen_US
dc.subjectAprepitanten_US
dc.subjectChemotherapy-Induced Nauseaen_US
dc.subjectDrug-Deliveryen_US
dc.subjectBioavailability Enhancementen_US
dc.subjectSystemsen_US
dc.subjectDesignen_US
dc.subjectSeddsen_US
dc.subjectPreventionen_US
dc.subjectLipolysisen_US
dc.subjectSneddsen_US
dc.titleA Novel Semi-Solid Self-Emulsifying Formulation of Aprepitant for Oral Delivery: An In Vitro Evaluationen_US
dc.typeArticleen_US

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