Cargando…
Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility
BACKGROUND: The objective of this study was to evaluate fluid-bed coating as a new technique to prepare a pellet-based solid self-nanoemulsifying drug delivery system (SNEDDS) using cyclosporin A as a model of a poorly water-soluble drug. METHODS: The rationale of this technique was to entrap a Liqu...
Autores principales: | , , , , , , |
---|---|
Formato: | Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2011
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3090276/ https://www.ncbi.nlm.nih.gov/pubmed/21589647 http://dx.doi.org/10.2147/IJN.S17711 |
_version_ | 1782203126562947072 |
---|---|
author | Lei, Yang Lu, Yi Qi, Jianping Nie, Sufang Hu, Fuqiang Pan, Weisan Wu, Wei |
author_facet | Lei, Yang Lu, Yi Qi, Jianping Nie, Sufang Hu, Fuqiang Pan, Weisan Wu, Wei |
author_sort | Lei, Yang |
collection | PubMed |
description | BACKGROUND: The objective of this study was to evaluate fluid-bed coating as a new technique to prepare a pellet-based solid self-nanoemulsifying drug delivery system (SNEDDS) using cyclosporin A as a model of a poorly water-soluble drug. METHODS: The rationale of this technique was to entrap a Liquid SNEDDS in the matrix of the coating material, polyvinylpyrrolidone K30, by fluid-bed coating. Pseudoternary phase diagrams were used to screen the liquid SNEDDS formulations. The optimal formulation was composed of Labrafil M(®) 1944 CS, Transcutol P(®), and Cremophor(®) EL in a ratio of 9:14:7. To prepare solid SNEDDS pellets, liquid SNEDDS was first dispersed in an aqueous solution of polyvinylpyrrolidone and then sprayed onto the surface of non-pareil pellets. Upon evaporation of water, polyvinylpyrrolidone precipitated and formed tight films to entrap the liquid SNEDDS. Visual observation and scanning electron microscopic analysis confirmed good appearance of the solid SNEDDS pellets. RESULTS: Our results indicated that up to 40% of the liquid SNEDDS could be entrapped in the coating layer. Powder x-ray diffraction analysis confirmed nonexistence of crystalline cyclosporin A in the formulation. Solid SNEDDS pellets showed a slower redispersion rate than the liquid SNEDDS. An increase in the total liquid SNEDDS loading led to faster redispersion, whereas increased coating weight (up to 400%) significantly decreased the redispersion rate. Both cyclosporin A loading and protective coating with 5% polyvinylpyrrolidone K30 did not significantly affect the redispersion rate. CONCLUSION: It is concluded that fluid-bed coating is a new technique with considerable potential for preparation of pellet-based solid SNEDDS formulations. |
format | Text |
id | pubmed-3090276 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-30902762011-05-17 Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility Lei, Yang Lu, Yi Qi, Jianping Nie, Sufang Hu, Fuqiang Pan, Weisan Wu, Wei Int J Nanomedicine Original Research BACKGROUND: The objective of this study was to evaluate fluid-bed coating as a new technique to prepare a pellet-based solid self-nanoemulsifying drug delivery system (SNEDDS) using cyclosporin A as a model of a poorly water-soluble drug. METHODS: The rationale of this technique was to entrap a Liquid SNEDDS in the matrix of the coating material, polyvinylpyrrolidone K30, by fluid-bed coating. Pseudoternary phase diagrams were used to screen the liquid SNEDDS formulations. The optimal formulation was composed of Labrafil M(®) 1944 CS, Transcutol P(®), and Cremophor(®) EL in a ratio of 9:14:7. To prepare solid SNEDDS pellets, liquid SNEDDS was first dispersed in an aqueous solution of polyvinylpyrrolidone and then sprayed onto the surface of non-pareil pellets. Upon evaporation of water, polyvinylpyrrolidone precipitated and formed tight films to entrap the liquid SNEDDS. Visual observation and scanning electron microscopic analysis confirmed good appearance of the solid SNEDDS pellets. RESULTS: Our results indicated that up to 40% of the liquid SNEDDS could be entrapped in the coating layer. Powder x-ray diffraction analysis confirmed nonexistence of crystalline cyclosporin A in the formulation. Solid SNEDDS pellets showed a slower redispersion rate than the liquid SNEDDS. An increase in the total liquid SNEDDS loading led to faster redispersion, whereas increased coating weight (up to 400%) significantly decreased the redispersion rate. Both cyclosporin A loading and protective coating with 5% polyvinylpyrrolidone K30 did not significantly affect the redispersion rate. CONCLUSION: It is concluded that fluid-bed coating is a new technique with considerable potential for preparation of pellet-based solid SNEDDS formulations. Dove Medical Press 2011 2011-04-19 /pmc/articles/PMC3090276/ /pubmed/21589647 http://dx.doi.org/10.2147/IJN.S17711 Text en © 2011 Lei et al, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited. |
spellingShingle | Original Research Lei, Yang Lu, Yi Qi, Jianping Nie, Sufang Hu, Fuqiang Pan, Weisan Wu, Wei Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility |
title | Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility |
title_full | Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility |
title_fullStr | Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility |
title_full_unstemmed | Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility |
title_short | Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility |
title_sort | solid self-nanoemulsifying cyclosporin a pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3090276/ https://www.ncbi.nlm.nih.gov/pubmed/21589647 http://dx.doi.org/10.2147/IJN.S17711 |
work_keys_str_mv | AT leiyang solidselfnanoemulsifyingcyclosporinapelletspreparedbyfluidbedcoatingpreparationcharacterizationandinvitroredispersibility AT luyi solidselfnanoemulsifyingcyclosporinapelletspreparedbyfluidbedcoatingpreparationcharacterizationandinvitroredispersibility AT qijianping solidselfnanoemulsifyingcyclosporinapelletspreparedbyfluidbedcoatingpreparationcharacterizationandinvitroredispersibility AT niesufang solidselfnanoemulsifyingcyclosporinapelletspreparedbyfluidbedcoatingpreparationcharacterizationandinvitroredispersibility AT hufuqiang solidselfnanoemulsifyingcyclosporinapelletspreparedbyfluidbedcoatingpreparationcharacterizationandinvitroredispersibility AT panweisan solidselfnanoemulsifyingcyclosporinapelletspreparedbyfluidbedcoatingpreparationcharacterizationandinvitroredispersibility AT wuwei solidselfnanoemulsifyingcyclosporinapelletspreparedbyfluidbedcoatingpreparationcharacterizationandinvitroredispersibility |