Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation
Introduction: Insulin is given by injection, because when administered orally, it would be destroyed by enzymes in the digestive system, hence only about 0.1% reaches blood circulation. The purpose of the present study was to use pH sensitive polyelectrolyte methyl methacrylate (MMA)/itaconic acid (...
| 主要な著者: | , , , |
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| フォーマット: | 論文 |
| 言語: | English |
| 出版事項: |
Dovepress
2019
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| 主題: | |
| オンライン･アクセス: | http://umpir.ump.edu.my/id/eprint/27329/1/Self-assembled%20insulin%20and%20nanogels%20polyelectrolyte%20complex.pdf |
| _version_ | 1825813145997803520 |
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| author | Mudassir, Jahanzeb Yusrida, Darwis Suriani, Muhamad Khan, Arshad Ali |
| author_facet | Mudassir, Jahanzeb Yusrida, Darwis Suriani, Muhamad Khan, Arshad Ali |
| author_sort | Mudassir, Jahanzeb |
| collection | UMP |
| description | Introduction: Insulin is given by injection, because when administered orally, it would be destroyed by enzymes in the digestive system, hence only about 0.1% reaches blood circulation. The purpose of the present study was to use pH sensitive polyelectrolyte methyl methacrylate (MMA)/itaconic acid (IA) nanogels as carriers in an attempt to improve absorption of insulin administered orally. Methods: Insulin (Ins) was incorporated into the MMA/IA nanogels (NGs) using the polyelectrolyte complexation (PEC) method to form Ins/NGs-PEC. Several parameters, including Ins:NGs ratio, pH, incubation time and stirring rate were optimized during preparation of InsNGs-PEC. The prepared formulations were characterized in terms of particle size (PS), polydispersity index (PdI), zeta potential (ZP) and percent entrapment efficiency (% EE). Results: The optimized InF12 nanogels had a PS, PdI, ZP and %EE of 190.43 nm, 0.186, −16.70 mV and 85.20%, respectively. The InF12 nanogels were lyophilized in the presence of different concentrations of trehalose as cryoprotectant. The lyophilized InF12 containing 2%w/v trahalose (InF12-Tre2 nanogels) was chosen as final formulation which had a PS, PdI, ZP and %EE of 430.50 nm, 0.588, −16.50 mv and 82.10, respectively. The in vitro release of insulin from InF12-Tre2 nanogels in the SGF and SIF were 28.71% and 96.53%, respectively. The stability study conducted at 5±3°C for 3 months showed that lnF12-Tre2 nanogels were stable. The SDS-PAGE assay indicated that the primary structure of insulin in the lnF12-Tre2 nanogels was intact. The in-vivo study in the diabetic rats following oral administration of InF12-Tre2 nanogels at a dose of 100 IU/kg body weight reduced blood glucose level significantly to 51.10% after 6 hours compared to the control groups. Conclusions: The pH sensitive MMA/IA nanogels are potential carriers for oral delivery of insulin as they enhanced the absorption of the drug. |
| first_indexed | 2024-03-06T12:39:41Z |
| format | Article |
| id | UMPir27329 |
| institution | Universiti Malaysia Pahang |
| language | English |
| last_indexed | 2024-03-06T12:39:41Z |
| publishDate | 2019 |
| publisher | Dovepress |
| record_format | dspace |
| spelling | UMPir273292020-03-29T23:16:11Z http://umpir.ump.edu.my/id/eprint/27329/ Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation Mudassir, Jahanzeb Yusrida, Darwis Suriani, Muhamad Khan, Arshad Ali R Medicine (General) RM Therapeutics. Pharmacology TP Chemical technology Introduction: Insulin is given by injection, because when administered orally, it would be destroyed by enzymes in the digestive system, hence only about 0.1% reaches blood circulation. The purpose of the present study was to use pH sensitive polyelectrolyte methyl methacrylate (MMA)/itaconic acid (IA) nanogels as carriers in an attempt to improve absorption of insulin administered orally. Methods: Insulin (Ins) was incorporated into the MMA/IA nanogels (NGs) using the polyelectrolyte complexation (PEC) method to form Ins/NGs-PEC. Several parameters, including Ins:NGs ratio, pH, incubation time and stirring rate were optimized during preparation of InsNGs-PEC. The prepared formulations were characterized in terms of particle size (PS), polydispersity index (PdI), zeta potential (ZP) and percent entrapment efficiency (% EE). Results: The optimized InF12 nanogels had a PS, PdI, ZP and %EE of 190.43 nm, 0.186, −16.70 mV and 85.20%, respectively. The InF12 nanogels were lyophilized in the presence of different concentrations of trehalose as cryoprotectant. The lyophilized InF12 containing 2%w/v trahalose (InF12-Tre2 nanogels) was chosen as final formulation which had a PS, PdI, ZP and %EE of 430.50 nm, 0.588, −16.50 mv and 82.10, respectively. The in vitro release of insulin from InF12-Tre2 nanogels in the SGF and SIF were 28.71% and 96.53%, respectively. The stability study conducted at 5±3°C for 3 months showed that lnF12-Tre2 nanogels were stable. The SDS-PAGE assay indicated that the primary structure of insulin in the lnF12-Tre2 nanogels was intact. The in-vivo study in the diabetic rats following oral administration of InF12-Tre2 nanogels at a dose of 100 IU/kg body weight reduced blood glucose level significantly to 51.10% after 6 hours compared to the control groups. Conclusions: The pH sensitive MMA/IA nanogels are potential carriers for oral delivery of insulin as they enhanced the absorption of the drug. Dovepress 2019-07-05 Article PeerReviewed pdf en cc_by_nc http://umpir.ump.edu.my/id/eprint/27329/1/Self-assembled%20insulin%20and%20nanogels%20polyelectrolyte%20complex.pdf Mudassir, Jahanzeb and Yusrida, Darwis and Suriani, Muhamad and Khan, Arshad Ali (2019) Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation. International Journal of Nanomedicine, 14. pp. 4895-4909. ISSN 1178-2013. (Published) https://doi.org/10.2147/IJN.S199507 https://doi.org/10.2147/IJN.S199507 |
| spellingShingle | R Medicine (General) RM Therapeutics. Pharmacology TP Chemical technology Mudassir, Jahanzeb Yusrida, Darwis Suriani, Muhamad Khan, Arshad Ali Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation |
| title | Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation |
| title_full | Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation |
| title_fullStr | Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation |
| title_full_unstemmed | Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation |
| title_short | Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: Characterization, lyophilization and in-vivo evaluation |
| title_sort | self assembled insulin and nanogels polyelectrolyte complex ins ngs pec for oral insulin delivery characterization lyophilization and in vivo evaluation |
| topic | R Medicine (General) RM Therapeutics. Pharmacology TP Chemical technology |
| url | http://umpir.ump.edu.my/id/eprint/27329/1/Self-assembled%20insulin%20and%20nanogels%20polyelectrolyte%20complex.pdf |
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