Full Text from SpringerLink Lipospheres for Simultaneous Controlled Release and Improved Pharmacokinetic Profiles of Saxagliptin-Enalapril: Formulation, Optimization, and Comparative In Vitro-In Vivo Evaluation.
| Title: | Lipospheres for Simultaneous Controlled Release and Improved Pharmacokinetic Profiles of Saxagliptin-Enalapril: Formulation, Optimization, and Comparative In Vitro-In Vivo Evaluation. |
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| Authors: | Maheen, Safirah, Rasul, Akhtar, Hanif, Muhammad, Khan, Hafeez Ullah |
| Source: | AAPS PharmSciTech; Jul2020, Vol. 21 Issue 5, p1-16, 16p |
| Abstract: | The current study aims at formulating and optimizing lipospheres (LS) by the Box-Behnken design (BBD) from safe biodegradable carnauba wax (CW) to co-administer saxagliptin (SG) and enalapril (EP) for co-existing chronic hypertensive diabetes in order to overcome inadequacies of conventional modes of drug administration. Optimized liposphere formulation (OLF) was selected by a numerical optimization procedure and a comparative in vivo pharmacokinetic study of OLF and commercial brands was also performed. Discrete, free-flowing, spherical, smooth-surface LS having a size range of 5–10 μm and zeta potential of − 20 to − 30 mV were successfully formulated. Compatibility studies by FTIR and DSC proved the lack of interaction of components while XRD suggested the transformation of crystalline drugs to amorphous form. Outcomes of dependent optimizing variables like percentage yield (30–90%), EP-release (32–92%), and SG-release (28–95%) followed a polynomial quadratic model. Pharmacokinetics studies indicated a significantly lower C |
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| Database: | Complementary Index |
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| Header | DbId: edb DbLabel: Complementary Index An: 144509795 RelevancyScore: 915 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 915.358642578125 |
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| Items | – Name: Title Label: Title Group: Ti Data: Lipospheres for Simultaneous Controlled Release and Improved Pharmacokinetic Profiles of Saxagliptin-Enalapril: Formulation, Optimization, and Comparative In Vitro-In Vivo Evaluation. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Maheen%2C+Safirah%22">Maheen, Safirah</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> – Name: TitleSource Label: Source Group: Src Data: AAPS PharmSciTech; Jul2020, Vol. 21 Issue 5, p1-16, 16p – Name: Abstract Label: Abstract Group: Ab Data: The current study aims at formulating and optimizing lipospheres (LS) by the Box-Behnken design (BBD) from safe biodegradable carnauba wax (CW) to co-administer saxagliptin (SG) and enalapril (EP) for co-existing chronic hypertensive diabetes in order to overcome inadequacies of conventional modes of drug administration. Optimized liposphere formulation (OLF) was selected by a numerical optimization procedure and a comparative in vivo pharmacokinetic study of OLF and commercial brands was also performed. Discrete, free-flowing, spherical, smooth-surface LS having a size range of 5–10 μm and zeta potential of − 20 to − 30 mV were successfully formulated. Compatibility studies by FTIR and DSC proved the lack of interaction of components while XRD suggested the transformation of crystalline drugs to amorphous form. Outcomes of dependent optimizing variables like percentage yield (30–90%), EP-release (32–92%), and SG-release (28–95%) followed a polynomial quadratic model. Pharmacokinetics studies indicated a significantly lower C<subscript>max</subscript> of EP (125.22 ± 6.32) and SG (75.63 ± 3.85) and higher mean T<subscript>max</subscript> values (9.4 h for EP and 10.73 h for SG) from OLF in comparison with reference brands of EP (257.54 ± 8.23 ng/mL) and SG (393.66 ± 2.97 ng/mL). Additionally, a potential rise in half-life and MRT of SG and EP was achieved reaching approximately 2- to 3-fold higher than noted for reference brands. Importantly, the enhanced T<subscript>max</subscript> and AUC<subscript>0–24</subscript> specified the achievement of enhanced bioavailability of both drugs from LS. Consequently, such an innovative approach could not only control drug release in both in vitro and in vivo analyses but also maintain plasma drug concentration for a longer time without maximizing C<subscript>max</subscript> leading towards effective management of chronic illnesses. [ABSTRACT FROM AUTHOR] – Name: Abstract Label: Group: Ab Data: <i>Copyright of AAPS PharmSciTech is the property of Springer Nature 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: 10.1208/s12249-020-01733-w Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 16 StartPage: 1 Titles: – TitleFull: Lipospheres for Simultaneous Controlled Release and Improved Pharmacokinetic Profiles of Saxagliptin-Enalapril: Formulation, Optimization, and Comparative In Vitro-In Vivo Evaluation. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Maheen, Safirah – PersonEntity: Name: NameFull: Rasul, Akhtar – PersonEntity: Name: NameFull: Hanif, Muhammad – PersonEntity: Name: NameFull: Khan, Hafeez Ullah IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 07 Text: Jul2020 Type: published Y: 2020 Identifiers: – Type: issn-print Value: 15309932 Numbering: – Type: volume Value: 21 – Type: issue Value: 5 Titles: – TitleFull: AAPS PharmSciTech Type: main |
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