Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS).
| Title: | Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS). |
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| Authors: | Ashfaq, Mehran, Shah, Shahid, Rasul, Akhtar, Hanif, Muhammad, Khan, Hafeez Ullah, Khames, Ahmed, Abdelgawad, Mohamed A., Ghoneim, Mohammed M., Ali, Muhammad Yasir, Abourehab, Mohammad A. S., Maheen, Safirah, Iqbal, Omeira, Abbas, Ghulam, El Sisi, Amani M. |
| Source: | Pharmaceutics; Mar2022, Vol. 14 Issue 3, p482, 18p |
| Subject Terms: | DRUG solubility, DRUG delivery systems, PITAVASTATIN, SOLUBILITY, EMULSIONS (Pharmacy), BIOAVAILABILITY, ZETA potential, PHASE diagrams |
| Abstract: | The purpose of the study was to develop an SNEDDS to improve the solubility and bioavailability of pitavastatin. The solubility of pitavastatin in different oils, surfactants, and co-surfactants was determined and a pseudo-ternary phase diagram was constructed. The SNEDDS was characterized by zeta-sizer, zeta-potential, FTIR, DSC, and TGA. Release and permeation of pitavastatin from the SNEDDS was studied for 12 and 24 h, respectively. The lipolysis test, RBC lysis, effect on lipid profile, and pharmacokinetics were studied. The SPC3 formulation showed a 104 ± 1.50 nm particle size, a 0.198 polydispersity index (PDI), and a –29 zeta potential. FTIR, DSC, and TGA showed the chemical compatibility and thermal stability. The release and permeation of pitavastatin from SPC3 was 88.5 ± 2.5% and 96%, respectively. In the lipolysis test, the digestion of SPC3 yielded a high amount of pitavastatin and showed little RBC lysis. The lipid profile suggested that after 35 days of administration of the SNEDDS, there was a marked decrease in TC, LDL, and triglyceride levels. The SNEDDS of SPC3 showed an 86% viability of Caco-2 cells. Pharmacokinetics of SPC3 showed improved values of C |
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| Database: | Complementary Index |
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| Header | DbId: edb DbLabel: Complementary Index An: 156072441 RelevancyScore: 938 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 937.570434570313 |
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| Items | – Name: Title Label: Title Group: Ti Data: Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS). – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Ashfaq%2C+Mehran%22">Ashfaq, Mehran</searchLink><br /><searchLink fieldCode="AR" term="%22Shah%2C+Shahid%22">Shah, Shahid</searchLink><br /><searchLink fieldCode="AR" term="%22Rasul%2C+Akhtar%22">Rasul, Akhtar</searchLink><br /><searchLink fieldCode="AR" term="%22Hanif%2C+Muhammad%22">Hanif, Muhammad</searchLink><br /><searchLink fieldCode="AR" term="%22Khan%2C+Hafeez+Ullah%22">Khan, Hafeez Ullah</searchLink><br /><searchLink fieldCode="AR" term="%22Khames%2C+Ahmed%22">Khames, Ahmed</searchLink><br /><searchLink fieldCode="AR" term="%22Abdelgawad%2C+Mohamed+A%2E%22">Abdelgawad, Mohamed A.</searchLink><br /><searchLink fieldCode="AR" term="%22Ghoneim%2C+Mohammed+M%2E%22">Ghoneim, Mohammed M.</searchLink><br /><searchLink fieldCode="AR" term="%22Ali%2C+Muhammad+Yasir%22">Ali, Muhammad Yasir</searchLink><br /><searchLink fieldCode="AR" term="%22Abourehab%2C+Mohammad+A%2E+S%2E%22">Abourehab, Mohammad A. S.</searchLink><br /><searchLink fieldCode="AR" term="%22Maheen%2C+Safirah%22">Maheen, Safirah</searchLink><br /><searchLink fieldCode="AR" term="%22Iqbal%2C+Omeira%22">Iqbal, Omeira</searchLink><br /><searchLink fieldCode="AR" term="%22Abbas%2C+Ghulam%22">Abbas, Ghulam</searchLink><br /><searchLink fieldCode="AR" term="%22El+Sisi%2C+Amani+M%2E%22">El Sisi, Amani M.</searchLink> – Name: TitleSource Label: Source Group: Src Data: Pharmaceutics; Mar2022, Vol. 14 Issue 3, p482, 18p – Name: Subject Label: Subject Terms Group: Su Data: <searchLink fieldCode="DE" term="%22DRUG+solubility%22">DRUG solubility</searchLink><br /><searchLink fieldCode="DE" term="%22DRUG+delivery+systems%22">DRUG delivery systems</searchLink><br /><searchLink fieldCode="DE" term="%22PITAVASTATIN%22">PITAVASTATIN</searchLink><br /><searchLink fieldCode="DE" term="%22SOLUBILITY%22">SOLUBILITY</searchLink><br /><searchLink fieldCode="DE" term="%22EMULSIONS+%28Pharmacy%29%22">EMULSIONS (Pharmacy)</searchLink><br /><searchLink fieldCode="DE" term="%22BIOAVAILABILITY%22">BIOAVAILABILITY</searchLink><br /><searchLink fieldCode="DE" term="%22ZETA+potential%22">ZETA potential</searchLink><br /><searchLink fieldCode="DE" term="%22PHASE+diagrams%22">PHASE diagrams</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: The purpose of the study was to develop an SNEDDS to improve the solubility and bioavailability of pitavastatin. The solubility of pitavastatin in different oils, surfactants, and co-surfactants was determined and a pseudo-ternary phase diagram was constructed. The SNEDDS was characterized by zeta-sizer, zeta-potential, FTIR, DSC, and TGA. Release and permeation of pitavastatin from the SNEDDS was studied for 12 and 24 h, respectively. The lipolysis test, RBC lysis, effect on lipid profile, and pharmacokinetics were studied. The SPC3 formulation showed a 104 ± 1.50 nm particle size, a 0.198 polydispersity index (PDI), and a –29 zeta potential. FTIR, DSC, and TGA showed the chemical compatibility and thermal stability. The release and permeation of pitavastatin from SPC3 was 88.5 ± 2.5% and 96%, respectively. In the lipolysis test, the digestion of SPC3 yielded a high amount of pitavastatin and showed little RBC lysis. The lipid profile suggested that after 35 days of administration of the SNEDDS, there was a marked decrease in TC, LDL, and triglyceride levels. The SNEDDS of SPC3 showed an 86% viability of Caco-2 cells. Pharmacokinetics of SPC3 showed improved values of C<subscript>max</subscript>, T<subscript>max</subscript>, half-life, MRT, AUC, and AUMC compared to the reference formulation. Our study demonstrated that the SNEDDS effectively enhanced the solubility and bioavailability of a BCS class II drug. [ABSTRACT FROM AUTHOR] – Name: Abstract Label: Group: Ab Data: <i>Copyright of Pharmaceutics is the property of MDPI and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
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| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.3390/pharmaceutics14030482 Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 18 StartPage: 482 Subjects: – SubjectFull: DRUG solubility Type: general – SubjectFull: DRUG delivery systems Type: general – SubjectFull: PITAVASTATIN Type: general – SubjectFull: SOLUBILITY Type: general – SubjectFull: EMULSIONS (Pharmacy) Type: general – SubjectFull: BIOAVAILABILITY Type: general – SubjectFull: ZETA potential Type: general – SubjectFull: PHASE diagrams Type: general Titles: – TitleFull: Enhancement of the Solubility and Bioavailability of Pitavastatin through a Self-Nanoemulsifying Drug Delivery System (SNEDDS). Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Ashfaq, Mehran – PersonEntity: Name: NameFull: Shah, Shahid – PersonEntity: Name: NameFull: Rasul, Akhtar – PersonEntity: Name: NameFull: Hanif, Muhammad – PersonEntity: Name: NameFull: Khan, Hafeez Ullah – PersonEntity: Name: NameFull: Khames, Ahmed – PersonEntity: Name: NameFull: Abdelgawad, Mohamed A. – PersonEntity: Name: NameFull: Ghoneim, Mohammed M. – PersonEntity: Name: NameFull: Ali, Muhammad Yasir – PersonEntity: Name: NameFull: Abourehab, Mohammad A. S. – PersonEntity: Name: NameFull: Maheen, Safirah – PersonEntity: Name: NameFull: Iqbal, Omeira – PersonEntity: Name: NameFull: Abbas, Ghulam – PersonEntity: Name: NameFull: El Sisi, Amani M. IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 03 Text: Mar2022 Type: published Y: 2022 Identifiers: – Type: issn-print Value: 19994923 Numbering: – Type: volume Value: 14 – Type: issue Value: 3 Titles: – TitleFull: Pharmaceutics Type: main |
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