Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex
AbstractIn present, there was no detailed report on the formulation optimization and quality evaluation of aprepitant (APT) injectable lipid emulsion (APT-IE). The aim of the present investigation was to prepare and evaluate its properties of APT-IE loaded with an APT phospholipid complex (APT-PC) i...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2023-12-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2023.2183834 |
| _version_ | 1797260957393616896 |
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| author | Yan Li Hong Yin Chensi Wu Jia He Chunyan Wang Bo Ren Heping Wang Dandan Geng Yirong Zhang Ligang Zhao |
| author_facet | Yan Li Hong Yin Chensi Wu Jia He Chunyan Wang Bo Ren Heping Wang Dandan Geng Yirong Zhang Ligang Zhao |
| author_sort | Yan Li |
| collection | DOAJ |
| description | AbstractIn present, there was no detailed report on the formulation optimization and quality evaluation of aprepitant (APT) injectable lipid emulsion (APT-IE). The aim of the present investigation was to prepare and evaluate its properties of APT-IE loaded with an APT phospholipid complex (APT-PC) in vitro and in vivo. APT-PC was obtained by solvent evaporation with APT and phospholipids, then analyzed by X-ray diffraction, Fourier transform infrared spectroscopy and differential scanning calorimetry. Lipid emulsions are a new formulation that can reduce side effects and improve drug loading.APT-IE prepared by High-pressure homogenization and optimized by response surface methodology (RSM). The proportion of sodium oleate, poloxamer 188 and soybean oil were selected as variables for the optimization. The optimal formulation of ATP-IE had the following characteristics: particle size, 82.83 ± 1.89 nm; polydispersity index, 0.243 ± 0.008; zeta potential, −59.0 ± 2.54 mV; encapsulation efficiency, 98.84%±1.43%; drug loading, 7.08 ± 0.16 mg/mL; and osmotic pressure, 301 ± 2.15 mOsmol/kg. Transmission electron microscopy images indicated that the particle diameter of APT-IE was approximately 100 nm, with a morphology of spheroidal or spherical. APT-IE exhibited sufficient stability after storage at 4 ± 2 °C for more than 6 months. The results of the pharmacokinetic study demonstrated that APT-IE had the advantages of better safety, higher bioavailability, and obvious liver targeting than APT solution (APT-SL). The area under the curve (AUC) of APT-IE was 3-fold enhanced compared with APT-SL. The targeted enhancement multiple of APT-IE to liver tissue was greater than that of APT-SL. These results suggested that APT-IE has broad clinical application and industrial production potential. |
| first_indexed | 2024-03-08T23:30:57Z |
| format | Article |
| id | doaj.art-a8d8ff6e57a64fc2babd881dee0c3747 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-04-24T23:33:34Z |
| publishDate | 2023-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-a8d8ff6e57a64fc2babd881dee0c37472024-03-15T14:22:18ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642023-12-0130110.1080/10717544.2023.2183834Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complexYan Li0Hong Yin1Chensi Wu2Jia He3Chunyan Wang4Bo Ren5Heping Wang6Dandan Geng7Yirong Zhang8Ligang Zhao9Department of Pharmacy, Tangshan Maternal and Child Health Hospital, Tangshan, ChinaSchool of Pharmacy, North China University of Science and Technology, Tangshan, ChinaSchool of Pharmacy, North China University of Science and Technology, Tangshan, ChinaDepartment of Pharmacy, Hohhot Hospital of Traditional Chinese Medicine and Mongolian Medicine, Hohhot, ChinaDepartment of Pharmacy, Tangshan Maternal and Child Health Hospital, Tangshan, ChinaSchool of Pharmacy, North China University of Science and Technology, Tangshan, ChinaSchool of Pharmacy, North China University of Science and Technology, Tangshan, ChinaSchool of Pharmacy, North China University of Science and Technology, Tangshan, ChinaSchool of Pharmacy, North China University of Science and Technology, Tangshan, ChinaSchool of Pharmacy, North China University of Science and Technology, Tangshan, ChinaAbstractIn present, there was no detailed report on the formulation optimization and quality evaluation of aprepitant (APT) injectable lipid emulsion (APT-IE). The aim of the present investigation was to prepare and evaluate its properties of APT-IE loaded with an APT phospholipid complex (APT-PC) in vitro and in vivo. APT-PC was obtained by solvent evaporation with APT and phospholipids, then analyzed by X-ray diffraction, Fourier transform infrared spectroscopy and differential scanning calorimetry. Lipid emulsions are a new formulation that can reduce side effects and improve drug loading.APT-IE prepared by High-pressure homogenization and optimized by response surface methodology (RSM). The proportion of sodium oleate, poloxamer 188 and soybean oil were selected as variables for the optimization. The optimal formulation of ATP-IE had the following characteristics: particle size, 82.83 ± 1.89 nm; polydispersity index, 0.243 ± 0.008; zeta potential, −59.0 ± 2.54 mV; encapsulation efficiency, 98.84%±1.43%; drug loading, 7.08 ± 0.16 mg/mL; and osmotic pressure, 301 ± 2.15 mOsmol/kg. Transmission electron microscopy images indicated that the particle diameter of APT-IE was approximately 100 nm, with a morphology of spheroidal or spherical. APT-IE exhibited sufficient stability after storage at 4 ± 2 °C for more than 6 months. The results of the pharmacokinetic study demonstrated that APT-IE had the advantages of better safety, higher bioavailability, and obvious liver targeting than APT solution (APT-SL). The area under the curve (AUC) of APT-IE was 3-fold enhanced compared with APT-SL. The targeted enhancement multiple of APT-IE to liver tissue was greater than that of APT-SL. These results suggested that APT-IE has broad clinical application and industrial production potential.https://www.tandfonline.com/doi/10.1080/10717544.2023.2183834Aprepitantlipid injectable emulsionresponse surface methodologypharmacokineticstissue distribution |
| spellingShingle | Yan Li Hong Yin Chensi Wu Jia He Chunyan Wang Bo Ren Heping Wang Dandan Geng Yirong Zhang Ligang Zhao Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex Drug Delivery Aprepitant lipid injectable emulsion response surface methodology pharmacokinetics tissue distribution |
| title | Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex |
| title_full | Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex |
| title_fullStr | Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex |
| title_full_unstemmed | Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex |
| title_short | Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex |
| title_sort | preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant phospholipid complex |
| topic | Aprepitant lipid injectable emulsion response surface methodology pharmacokinetics tissue distribution |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2023.2183834 |
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