Abstract：
:This paper reports for the first time the possible formation of a novel room temperature therapeutic deep eutectic solvent (THEDES) of risperidone (RIS) with some fatty acids, namely capric acid (C10; CA), lauric acid (C12; LA), and myristic acid (C14; MA). All mixtures of RIS and MA yielded a solid or pasty-like solid and were readily discarded. Some of the prepared THEDESs from RIS and CA or LA have spontaneously transformed into a transparent liquid, without any precipitate at room temperature by simple physical mixing of the components. From the DSC thermograms, phase diagrams of the eutectic systems were constructed and the lowest obtained melting point for a RIS:CA mixture was 17°C at 40:60% w/w ratio. While 22°C was recorded as the lowest melting point for RIS:LA at a ratio of 30:70% w/w, solubility improvement of RIS was up to 70,000-fold compared with water. Freeze-drying microscopy provided valuable information regarding the phase change and transitions the drug undergoes as a function of temperature and it clarifies the interpretation of the DSC results and provides valuable evidence of drug crystals co-melting within the fatty acid base. The presence of natural fatty acid as one component of THEDES and the depression in the melting point significantly (P < 0.05) enhanced RIS skin permeation. Rheological studies showed a viscosity temperature dependency of the DES and well fitted to the Arrhenius equation. Application of the obtained THEDES on the shaved skin of rats revealed the absence of any irritation or edema effects.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Al-Akayleh F,Adwan S,Khanfar M,Idkaidek N,Al-Remawi Mdoi
10.1208/s12249-020-01844-4subject
Has Abstractpub_date
2020-11-22 00:00:00pages
4issue
1issn
1530-9932pii
10.1208/s12249-020-01844-4journal_volume
22pub_type
杂志文章abstract：:The present study demonstrates a preparative medium-pressure liquid chromatography (MPLC) method for isolation of Morin besides evaluating its efficacy in comparison with its self-nanoemulsifying drug delivery (SNEDD) and nanoemulsion (NE) systems against in-vivo HgCl2-induced lung toxicity in rats. Morin was isolated...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-018-1072-6
更新日期：2018-07-01 00:00:00
abstract：:This proof-of-concept study explores the feasibility of using a drug-loaded hydrophilic polymeric layer sandwiched between two hydrophobic layers for improving film drug load while achieving sustained release of poorly water-soluble drug. Such films having total thickness in range ~ 146-250 μm were prepared by slurry-...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-018-1089-x
更新日期：2018-08-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt070105
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0223-7
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-1622-6
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journal_title：AAPS PharmSciTech
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doi：10.1208/s12249-019-1438-4
更新日期：2019-06-21 00:00:00
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-010-9464-2
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0205-9
更新日期：2015-02-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9091-3
更新日期：2008-01-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0282-9
更新日期：2015-08-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0418-6
更新日期：2016-08-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0566-3
更新日期：2017-02-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1581-y
更新日期：2019-12-23 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9165-2
更新日期：2008-01-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-010-9430-z
更新日期：2010-06-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0555-6
更新日期：2017-04-01 00:00:00
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01688-y
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0226-4
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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更新日期：2011-06-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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更新日期：2008-01-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-016-0543-x
更新日期：2016-08-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0505-3
更新日期：2017-02-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0081-3
更新日期：2014-06-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1382-3
更新日期：2019-07-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1361-8
更新日期：2019-03-26 00:00:00
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journal_title：AAPS PharmSciTech
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