Mohit Kumar, Pooja A. Chawla, Abdul Faruk and Viney Chawla
{"title":"具有优良吸附碱†的环孢素固体自纳米乳化给药系统的设计与评价","authors":"Mohit Kumar, Pooja A. Chawla, Abdul Faruk and Viney Chawla","doi":"10.1039/D4PM00198B","DOIUrl":null,"url":null,"abstract":"<p >Cyclosporine (CYC) is a drug that belongs to the BCS class II category. This study was designed to develop novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) for cyclosporine (CYC), using chitosan–EDTA microparticles. Such microparticles are known to exhibit superior adsorbent characteristics and were prepared by two different methods <em>viz</em>. spray drying (SD-CHEM) and solvent evaporation (SE-CHEM). Capmul® GMS-50K, Labrafac, and PEG 400 were chosen as the oil, surfactant, and co-surfactant, respectively. The cyclosporine liquid self-nanoemulsifying drug delivery system (CYC-L-SNEDDS) was developed with an optimal oil to <em>S</em><small><sub>mix</sub></small> (surfactant : co-surfactant) ratio of 40 : 60, determined through a pseudo ternary phase diagram. The novel S-SNEDDS were developed by adsorbing CYC-L-SNEDDS onto the chitosan–EDTA microparticles, resulting in CYC-SD-S-SNEDDS and CYC-SE-S-SNEDDS. Both formulations exhibited favorable drug loading, with 81.184 ± 4.191% for CYC-SD-S-SNEDDS and 56.426 ± 5.471% for CYC-SE-S-SNEDDS. XRD and DSC confirmed drug amorphization, while SEM revealed a smooth, well-distributed adsorbate on the adsorbent surfaces, with particle sizes of 5–8 μm for CYC-SD-S-SNEDDS and 10–12 μm for CYC-SE-S-SNEDDS. When tested for stability, the developed formulations exhibited excellent physical and thermodynamic stability. The globule size for CYC-SD-S-SNEDDS was 138.7 ± 4.14 nm, with a PDI of 0.613 ± 0.004, while CYC-SE-S-SNEDDS had a globule size of 166.9 ± 4.04 nm and a PDI of 0.579 ± 0.003. The results of <em>in vitro</em> dissolution studies revealed that there was a fourfold increase in drug dissolution for CYC-SD-S-SNEDDS (80.03%) and CYC-SE-S-SNEDDS (72.26%) when compared to the pure cyclosporine (19.8%). A similar pattern was observed in <em>ex vivo</em> permeation studies where CYC-SD-S-SNEDDS showed 39.34% release and CYC-SE-S-SNEDDS exhibited 28.31% release as compared to CYC-L-SNEDDS (41.46%). Furthermore, CYC-SD-S-SNEDDS outperformed CYC-SE-S-SNEDDS, indicating the superiority of microparticles developed by the spray drying method (SD-CHEM) as adsorbents for solidification. These findings suggest enhanced dissolution and permeation for cyclosporine in S-SNEDDS.</p>","PeriodicalId":101141,"journal":{"name":"RSC Pharmaceutics","volume":" 2","pages":" 318-332"},"PeriodicalIF":0.0000,"publicationDate":"2024-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00198b?page=search","citationCount":"0","resultStr":"{\"title\":\"Design and evaluation of solid self-nanoemulsifying drug delivery systems of cyclosporine developed with a superior adsorbent base†\",\"authors\":\"Mohit Kumar, Pooja A. Chawla, Abdul Faruk and Viney Chawla\",\"doi\":\"10.1039/D4PM00198B\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >Cyclosporine (CYC) is a drug that belongs to the BCS class II category. This study was designed to develop novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) for cyclosporine (CYC), using chitosan–EDTA microparticles. Such microparticles are known to exhibit superior adsorbent characteristics and were prepared by two different methods <em>viz</em>. spray drying (SD-CHEM) and solvent evaporation (SE-CHEM). Capmul® GMS-50K, Labrafac, and PEG 400 were chosen as the oil, surfactant, and co-surfactant, respectively. The cyclosporine liquid self-nanoemulsifying drug delivery system (CYC-L-SNEDDS) was developed with an optimal oil to <em>S</em><small><sub>mix</sub></small> (surfactant : co-surfactant) ratio of 40 : 60, determined through a pseudo ternary phase diagram. The novel S-SNEDDS were developed by adsorbing CYC-L-SNEDDS onto the chitosan–EDTA microparticles, resulting in CYC-SD-S-SNEDDS and CYC-SE-S-SNEDDS. Both formulations exhibited favorable drug loading, with 81.184 ± 4.191% for CYC-SD-S-SNEDDS and 56.426 ± 5.471% for CYC-SE-S-SNEDDS. XRD and DSC confirmed drug amorphization, while SEM revealed a smooth, well-distributed adsorbate on the adsorbent surfaces, with particle sizes of 5–8 μm for CYC-SD-S-SNEDDS and 10–12 μm for CYC-SE-S-SNEDDS. When tested for stability, the developed formulations exhibited excellent physical and thermodynamic stability. The globule size for CYC-SD-S-SNEDDS was 138.7 ± 4.14 nm, with a PDI of 0.613 ± 0.004, while CYC-SE-S-SNEDDS had a globule size of 166.9 ± 4.04 nm and a PDI of 0.579 ± 0.003. The results of <em>in vitro</em> dissolution studies revealed that there was a fourfold increase in drug dissolution for CYC-SD-S-SNEDDS (80.03%) and CYC-SE-S-SNEDDS (72.26%) when compared to the pure cyclosporine (19.8%). A similar pattern was observed in <em>ex vivo</em> permeation studies where CYC-SD-S-SNEDDS showed 39.34% release and CYC-SE-S-SNEDDS exhibited 28.31% release as compared to CYC-L-SNEDDS (41.46%). Furthermore, CYC-SD-S-SNEDDS outperformed CYC-SE-S-SNEDDS, indicating the superiority of microparticles developed by the spray drying method (SD-CHEM) as adsorbents for solidification. These findings suggest enhanced dissolution and permeation for cyclosporine in S-SNEDDS.</p>\",\"PeriodicalId\":101141,\"journal\":{\"name\":\"RSC Pharmaceutics\",\"volume\":\" 2\",\"pages\":\" 318-332\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-12-11\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://pubs.rsc.org/en/content/articlepdf/2025/pm/d4pm00198b?page=search\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"RSC Pharmaceutics\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://pubs.rsc.org/en/content/articlelanding/2025/pm/d4pm00198b\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"RSC Pharmaceutics","FirstCategoryId":"1085","ListUrlMain":"https://pubs.rsc.org/en/content/articlelanding/2025/pm/d4pm00198b","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Design and evaluation of solid self-nanoemulsifying drug delivery systems of cyclosporine developed with a superior adsorbent base†
Cyclosporine (CYC) is a drug that belongs to the BCS class II category. This study was designed to develop novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) for cyclosporine (CYC), using chitosan–EDTA microparticles. Such microparticles are known to exhibit superior adsorbent characteristics and were prepared by two different methods viz. spray drying (SD-CHEM) and solvent evaporation (SE-CHEM). Capmul® GMS-50K, Labrafac, and PEG 400 were chosen as the oil, surfactant, and co-surfactant, respectively. The cyclosporine liquid self-nanoemulsifying drug delivery system (CYC-L-SNEDDS) was developed with an optimal oil to Smix (surfactant : co-surfactant) ratio of 40 : 60, determined through a pseudo ternary phase diagram. The novel S-SNEDDS were developed by adsorbing CYC-L-SNEDDS onto the chitosan–EDTA microparticles, resulting in CYC-SD-S-SNEDDS and CYC-SE-S-SNEDDS. Both formulations exhibited favorable drug loading, with 81.184 ± 4.191% for CYC-SD-S-SNEDDS and 56.426 ± 5.471% for CYC-SE-S-SNEDDS. XRD and DSC confirmed drug amorphization, while SEM revealed a smooth, well-distributed adsorbate on the adsorbent surfaces, with particle sizes of 5–8 μm for CYC-SD-S-SNEDDS and 10–12 μm for CYC-SE-S-SNEDDS. When tested for stability, the developed formulations exhibited excellent physical and thermodynamic stability. The globule size for CYC-SD-S-SNEDDS was 138.7 ± 4.14 nm, with a PDI of 0.613 ± 0.004, while CYC-SE-S-SNEDDS had a globule size of 166.9 ± 4.04 nm and a PDI of 0.579 ± 0.003. The results of in vitro dissolution studies revealed that there was a fourfold increase in drug dissolution for CYC-SD-S-SNEDDS (80.03%) and CYC-SE-S-SNEDDS (72.26%) when compared to the pure cyclosporine (19.8%). A similar pattern was observed in ex vivo permeation studies where CYC-SD-S-SNEDDS showed 39.34% release and CYC-SE-S-SNEDDS exhibited 28.31% release as compared to CYC-L-SNEDDS (41.46%). Furthermore, CYC-SD-S-SNEDDS outperformed CYC-SE-S-SNEDDS, indicating the superiority of microparticles developed by the spray drying method (SD-CHEM) as adsorbents for solidification. These findings suggest enhanced dissolution and permeation for cyclosporine in S-SNEDDS.