A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers
A drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE...
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2021-03-01
|
| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/26/6/1809 |
| _version_ | 1797540314378928128 |
|---|---|
| author | Jifen Zhang Yanhua Wang Jirui Wang Tao Yi |
| author_facet | Jifen Zhang Yanhua Wang Jirui Wang Tao Yi |
| author_sort | Jifen Zhang |
| collection | DOAJ |
| description | A drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE by spray-drying. A series of water-soluble solid carriers were compared and then Box-Behnken design was used to optimize the parameters of spray-drying. The drug release and stability of the optimized solid NSSPE in vitro were also investigated. The results showed that hydroxypropyl-β-cyclodextrin (HP-β-CD), rather than solid carriers commonly used in solidification of traditional Pickering emulsions, was suitable for the solid NSSPE to retain the original appearance and size of emulsion droplets after reconstitution. The amount of HP-β-CD had more influences on the solid NSSPE than the feed rate and the inlet air temperature. Fluorescence microscopy, confocal laser scanning microscopy and scanning electron microscopy showed that the reconstituted emulsion of the solid NSSPE prepared with HP-β-CD had the same core-shell structure with a core of oil and a shell of puerarin nanocrystals as the liquid NSSPE. The particle size of puerarin nanocrystal sand interfacial adsorption rate also did not change significantly. The cumulative amount of released puerarin from the solid NSSPE had no significant difference compared with the liquid NSSPE, which were both significantly higher than that of puerarin crude material. The solid NSSPE was stable for 3 months under the accelerated condition of 75% relative humidity and 40 °C. Thus, it is possible todevelop the solid NSSPE preserving the unique microstructure and the superior properties in vitro of the liquid NSSPE for poorly soluble drugs. |
| first_indexed | 2024-03-10T12:59:17Z |
| format | Article |
| id | doaj.art-bdd599f979ab45a2b4356e3f9aca9b6a |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T12:59:17Z |
| publishDate | 2021-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-bdd599f979ab45a2b4356e3f9aca9b6a2023-11-21T11:41:01ZengMDPI AGMolecules1420-30492021-03-01266180910.3390/molecules26061809A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as CarriersJifen Zhang0Yanhua Wang1Jirui Wang2Tao Yi3College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, ChinaCollege of Pharmaceutical Sciences, Southwest University, Chongqing 400716, ChinaChongqing Academy of Chinese Materia Medica, Chongqing 400065, ChinaMacao Polytechnic Institute, School of Health Sciences and Sports, Macao 00853, ChinaA drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE by spray-drying. A series of water-soluble solid carriers were compared and then Box-Behnken design was used to optimize the parameters of spray-drying. The drug release and stability of the optimized solid NSSPE in vitro were also investigated. The results showed that hydroxypropyl-β-cyclodextrin (HP-β-CD), rather than solid carriers commonly used in solidification of traditional Pickering emulsions, was suitable for the solid NSSPE to retain the original appearance and size of emulsion droplets after reconstitution. The amount of HP-β-CD had more influences on the solid NSSPE than the feed rate and the inlet air temperature. Fluorescence microscopy, confocal laser scanning microscopy and scanning electron microscopy showed that the reconstituted emulsion of the solid NSSPE prepared with HP-β-CD had the same core-shell structure with a core of oil and a shell of puerarin nanocrystals as the liquid NSSPE. The particle size of puerarin nanocrystal sand interfacial adsorption rate also did not change significantly. The cumulative amount of released puerarin from the solid NSSPE had no significant difference compared with the liquid NSSPE, which were both significantly higher than that of puerarin crude material. The solid NSSPE was stable for 3 months under the accelerated condition of 75% relative humidity and 40 °C. Thus, it is possible todevelop the solid NSSPE preserving the unique microstructure and the superior properties in vitro of the liquid NSSPE for poorly soluble drugs.https://www.mdpi.com/1420-3049/26/6/1809nanocrystalsPickering emulsionssolid dosage formhydroxypropyl-β-cyclodextrinspray-dryingpuerarin |
| spellingShingle | Jifen Zhang Yanhua Wang Jirui Wang Tao Yi A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers Molecules nanocrystals Pickering emulsions solid dosage form hydroxypropyl-β-cyclodextrin spray-drying puerarin |
| title | A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers |
| title_full | A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers |
| title_fullStr | A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers |
| title_full_unstemmed | A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers |
| title_short | A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers |
| title_sort | novel solid nanocrystals self stabilized pickering emulsion prepared by spray drying with hydroxypropyl β cyclodextrin as carriers |
| topic | nanocrystals Pickering emulsions solid dosage form hydroxypropyl-β-cyclodextrin spray-drying puerarin |
| url | https://www.mdpi.com/1420-3049/26/6/1809 |
| work_keys_str_mv | AT jifenzhang anovelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers AT yanhuawang anovelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers AT jiruiwang anovelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers AT taoyi anovelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers AT jifenzhang novelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers AT yanhuawang novelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers AT jiruiwang novelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers AT taoyi novelsolidnanocrystalsselfstabilizedpickeringemulsionpreparedbyspraydryingwithhydroxypropylbcyclodextrinascarriers |