Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl
The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolutio...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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Universidade de São Paulo
2020-04-01
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| Series: | Brazilian Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100547&tlng=en |
| _version_ | 1811271373637550080 |
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| author | Hemangi Ramesh Trivedi Tanvi Mukund Siriah Prashant Keshao Puranik |
| author_facet | Hemangi Ramesh Trivedi Tanvi Mukund Siriah Prashant Keshao Puranik |
| author_sort | Hemangi Ramesh Trivedi |
| collection | DOAJ |
| description | The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L-SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability. |
| first_indexed | 2024-04-12T22:20:03Z |
| format | Article |
| id | doaj.art-ceb441172bee44f8950aee51ff09fa80 |
| institution | Directory Open Access Journal |
| issn | 2175-9790 |
| language | English |
| last_indexed | 2024-04-12T22:20:03Z |
| publishDate | 2020-04-01 |
| publisher | Universidade de São Paulo |
| record_format | Article |
| series | Brazilian Journal of Pharmaceutical Sciences |
| spelling | doaj.art-ceb441172bee44f8950aee51ff09fa802022-12-22T03:14:25ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences2175-97902020-04-015610.1590/s2175-97902019000418070Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HClHemangi Ramesh Trivedihttps://orcid.org/0000-0001-5547-8202Tanvi Mukund SiriahPrashant Keshao PuranikThe objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L-SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100547&tlng=enNebivolol hydrochlorideLiquid & Solid SMEDDSFull factorial designNeusilin US2 IR-SET |
| spellingShingle | Hemangi Ramesh Trivedi Tanvi Mukund Siriah Prashant Keshao Puranik Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl Brazilian Journal of Pharmaceutical Sciences Nebivolol hydrochloride Liquid & Solid SMEDDS Full factorial design Neusilin US2 IR-SET |
| title | Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
| title_full | Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
| title_fullStr | Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
| title_full_unstemmed | Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
| title_short | Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl |
| title_sort | experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol hcl |
| topic | Nebivolol hydrochloride Liquid & Solid SMEDDS Full factorial design Neusilin US2 IR-SET |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100547&tlng=en |
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