In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility

Aprepitant (APR) belongs to Class II of the Biopharmaceutical Classification System (BCS) because of its low aqueous solubility. The objective of the current work is to develop self-nanoemulsifying drug delivery systems (SNEDDS) of APR to enhance its aqueous solubility. Preformulation studies involv...

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Autores principales:	Hakan Nazlı, Burcu Mesut, Yıldız Özsoy
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	aprepitant supersaturated SNEDDS solid SNEDDS solubility enhancement soluplus<sup>®</sup> imwitor<sup>®</sup> 988 Medicine R Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/5372e58bda8f4188b6ff6eb7d2f6e099
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spelling	oai:doaj.org-article:5372e58bda8f4188b6ff6eb7d2f6e0992021-11-25T18:39:15ZIn Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility10.3390/ph141110891424-8247https://doaj.org/article/5372e58bda8f4188b6ff6eb7d2f6e0992021-10-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1089https://doaj.org/toc/1424-8247Aprepitant (APR) belongs to Class II of the Biopharmaceutical Classification System (BCS) because of its low aqueous solubility. The objective of the current work is to develop self-nanoemulsifying drug delivery systems (SNEDDS) of APR to enhance its aqueous solubility. Preformulation studies involving screening of excipients for solubility and emulsification efficiency were carried out. Pseudo ternary phase diagrams were constructed with blends of oil (Imwitor<sup>®</sup> 988), cosolvent (Transcutol<sup>®</sup> P), and various surfactants (Kolliphor<sup>®</sup> RH40, Kolliphor<sup>®</sup> ELP, Kolliphor<sup>®</sup> HS15). The prepared SNEDDS were characterized for droplet size and nanoemulsion stability after dilution. Supersaturated SNEDDS (super-SNEDDS) were prepared to increase the quantity of loaded APR into the formulations. HPMC, PVP, PVP/VA, and Soluplus<sup>®</sup> were used as polymeric precipitation inhibitors (PPI). PPIs were added to the formulations at 5% and 10% by weight. The influence of the PPIs on drug precipitation was investigated. In vitro lipolysis test was carried out to simulate digestion of formulations in the gastrointestinal tract. Optimized super-SNEDDS were formulated into free-flowing granules by adsorption on the porous carriers such as Neusilin<sup>®</sup> US2. In vitro dissolution studies of solid super-SNEDDS formulation revealed an increased dissolution rate of the drug due to enhanced solubility. Consequently, a formulation to improve the solubility and potentially bioavailability of the drug was developed.Hakan NazlıBurcu MesutYıldız ÖzsoyMDPI AGarticleaprepitantsupersaturated SNEDDSsolid SNEDDSsolubility enhancementsoluplus<sup>®</sup>imwitor<sup>®</sup> 988MedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1089, p 1089 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	aprepitant supersaturated SNEDDS solid SNEDDS solubility enhancement soluplus<sup>®</sup> imwitor<sup>®</sup> 988 Medicine R Pharmacy and materia medica RS1-441
spellingShingle	aprepitant supersaturated SNEDDS solid SNEDDS solubility enhancement soluplus<sup>®</sup> imwitor<sup>®</sup> 988 Medicine R Pharmacy and materia medica RS1-441 Hakan Nazlı Burcu Mesut Yıldız Özsoy In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility
description	Aprepitant (APR) belongs to Class II of the Biopharmaceutical Classification System (BCS) because of its low aqueous solubility. The objective of the current work is to develop self-nanoemulsifying drug delivery systems (SNEDDS) of APR to enhance its aqueous solubility. Preformulation studies involving screening of excipients for solubility and emulsification efficiency were carried out. Pseudo ternary phase diagrams were constructed with blends of oil (Imwitor<sup>®</sup> 988), cosolvent (Transcutol<sup>®</sup> P), and various surfactants (Kolliphor<sup>®</sup> RH40, Kolliphor<sup>®</sup> ELP, Kolliphor<sup>®</sup> HS15). The prepared SNEDDS were characterized for droplet size and nanoemulsion stability after dilution. Supersaturated SNEDDS (super-SNEDDS) were prepared to increase the quantity of loaded APR into the formulations. HPMC, PVP, PVP/VA, and Soluplus<sup>®</sup> were used as polymeric precipitation inhibitors (PPI). PPIs were added to the formulations at 5% and 10% by weight. The influence of the PPIs on drug precipitation was investigated. In vitro lipolysis test was carried out to simulate digestion of formulations in the gastrointestinal tract. Optimized super-SNEDDS were formulated into free-flowing granules by adsorption on the porous carriers such as Neusilin<sup>®</sup> US2. In vitro dissolution studies of solid super-SNEDDS formulation revealed an increased dissolution rate of the drug due to enhanced solubility. Consequently, a formulation to improve the solubility and potentially bioavailability of the drug was developed.
format	article
author	Hakan Nazlı Burcu Mesut Yıldız Özsoy
author_facet	Hakan Nazlı Burcu Mesut Yıldız Özsoy
author_sort	Hakan Nazlı
title	In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility
title_short	In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility
title_full	In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility
title_fullStr	In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility
title_full_unstemmed	In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility
title_sort	in vitro evaluation of a solid supersaturated self nanoemulsifying drug delivery system (super-snedds) of aprepitant for enhanced solubility
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/5372e58bda8f4188b6ff6eb7d2f6e099
work_keys_str_mv	AT hakannazlı invitroevaluationofasolidsupersaturatedselfnanoemulsifyingdrugdeliverysystemsupersneddsofaprepitantforenhancedsolubility AT burcumesut invitroevaluationofasolidsupersaturatedselfnanoemulsifyingdrugdeliverysystemsupersneddsofaprepitantforenhancedsolubility AT yıldızozsoy invitroevaluationofasolidsupersaturatedselfnanoemulsifyingdrugdeliverysystemsupersneddsofaprepitantforenhancedsolubility
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In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility

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