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- 검색키워드
- 저자 : Taekwang Keum (검색결과 2 건)
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Bashyal, Santosh,Seo, Jo-Eun,Keum, Taekwang,Noh, Gyubin,Choi, Young Wook,Lee, Sangkil Dove Medical Press 2018 International journal of nanomedicine Vol.13 No.-
<P><B>Background</B></P><P>Buccal delivery of insulin is still a challenging issue for the researchers due to the presence of permeability barrier (buccal mucosa) in the buccal cavity. The main objective of this study was to investigate the safety, effectiveness, and potential of various liposomes containing different bile salts to improve the permeation of insulin across in vitro TR146 buccal cell layers.</P><P><B>Methods</B></P><P>Elastic bilosomes containing soy lecithin and bile salt edge activators (sodium cholate [SC], sodium taurocholate [STC], sodium glycocholate [SGC], sodium deoxyglycocholate [SDGC], or sodium deoxytaurocholate [SDTC]) were fabricated by thin-film hydration method. The prepared liposomes were characterized, and in vitro permeation studies were performed. The fluorescein isothiocyanate-insulin-loaded elastic bilosomes were used to evaluate the quantitative and qualitative cellular uptake studies.</P><P><B>Results</B></P><P>The prepared elastic bilosomes had a particle size and an entrapment efficiency of ~140–150 nm and 66%–78%, respectively. SDGC-lipo (SDGC-incorporated liposome) was observed to be the most superior with an enhancement ratio (ER) of 5.24 (<I>P</I><0.001). The SC-incorporated liposome (SC-lipo) and SDTC-incorporated liposome (SDTC-lipo) also led to a significant enhancement with ERs of 3.20 and 3.10 (<I>P</I><0.05), respectively, compared with insulin solution. These results were further supported by quantitative and qualitative cellular uptake studies performed employing fluorescence-activated cell sorting analysis and confocal microscopy, respectively. The relative median fluorescence intensity values of elastic bilosomes were counted in the order of SDGC-lipo > SC-lipo > SDTC-lipo > SGC-incorporated liposome > STC-incorporated liposome, and similarity in the permeability profile of the employed elastic bilosomes was noted.</P><P><B>Conclusion</B></P><P>This study presents the employment of various derivatives of cholic acid-loaded elastic bilosomes as a promising strategy to enhance the permeation of insulin through buccal route.</P>
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Shrawani Lamichhane,Jo-Eun Seo,Taekwang Keum,Gyubin Noh,Santosh Bashyal,Seong-Wan Cho,Eun-Hee Lee,Sangkil Lee 대한약학회 2022 Archives of Pharmacal Research Vol.45 No.1
Improving the aqueous solubility of poorlysoluble compounds have been a major issue in the pharmaceuticalindustry. In the present study, binary amorphoussolid dispersions (SDs) of Coenzyme Q10 (CoQ 10 ), a biopharmaceuticsclassifi cation system (BCS) II compound andSoluplus ® were prepared to enhance the solubility and pharmacokineticproperties compared to crystalline CoQ 10 . SDswere prepared with diff erent ratios of CoQ 10 and Soluplus ®(1:3, 1:5, and 1:7) using spray drying technology, and thephysicochemical properties of the SDs were evaluated. X-raypowder diff raction, diff erential scanning calorimetry, andscanning electron microscopy suggested the conversion ofthe crystalline form of CoQ 10 to a binary amorphous systemin the SDs. Fourier transform infrared spectroscopy revealedno potential interactions between CoQ 10 and Soluplus ® . The solubility of the optimal SD formulation (SD 1:7)was approximately 9000-fold higher than that of crystallineCoQ 10, and the increment was Soluplus ® concentrationdependent. As a result, optimized SD 1:7 also showed significantly enhanced dissolution rate where maximum drugrelease was observed within 30 min in two diff erent dissolutionmedia. Moreover, in contrast to crystalline CoQ 10, CoQ 10 SDs showed improved pharmacokinetic parameters. Thus, the SD 1:7 formulation is expected to improve biopharmaceuticalproperties and therapeutic effi cacy of CoQ 10 .
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