Intraoral Film Containing Insulin-Phospholipid Microemulsion: Formulation and In Vivo Hypoglycemic Activity Study
| Autor: | Veinardi Suendo, Heni Rachmawati, Bernard Manuel Haryadi, Kusnandar Anggadiredja |
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| Rok vydání: | 2014 |
| Předmět: |
Polymers
Chemistry Pharmaceutical medicine.medical_treatment Analytical chemistry Phospholipid Administration Oral Pharmaceutical Science Polyethylene glycol Aquatic Science Glycerides Polyethylene Glycols Chitosan Mice chemistry.chemical_compound Drug Discovery Zeta potential medicine Animals Hypoglycemic Agents Insulin Microemulsion Particle Size Phospholipids Ecology Evolution Behavior and Systematics PEG 400 Drug Carriers Chromatography Ecology technology industry and agriculture General Medicine chemistry Emulsions Female Drug carrier Agronomy and Crop Science Research Article |
| Zdroj: | AAPS PharmSciTech. 16:692-703 |
| ISSN: | 1530-9932 |
| DOI: | 10.1208/s12249-014-0258-9 |
| Popis: | Non-invasive administration of insulin is expected for better diabetes mellitus therapy. In this report, we developed intraoral preparation for insulin. Insulin was encapsulated into nanocarrier using self-assembly emulsification process. To increase lipophilicity of insulin, it was dispersed in phospholipid resulted in insulin-phospholipid solid dispersion. The microemulsion formula was established from our previous work which contained glyceryl monooleate (GMO), Tween 20, and polyethylene glycol (PEG 400) in a ratio of 1:8:1. To confirm the formation of insulin-phospholipid solid dispersion, PXRD, FTIR spectroscopy, and Raman spectroscopy were performed. Then, the microemulsion was evaluated for droplet size and distribution, zeta potential, entrapment efficiency, physical stability, and Raman spectroscopy. In addition, microemulsion with expected characteristic was evaluated for in vitro release, in vitro permeation, and in vivo activity. The droplets size of ∼100 nm with narrow distribution and positive charge of +0.56 mV were formed. The insulin encapsulated in the oil droplet was accounted of >90%. Water-soluble chitosan seems to be a promising film matrix polymer which also functioned as insulin release controller. Oral administration of insulin microemulsion to healthy Swiss-Webster mice showed hypoglycemic effect indicating the success of this protein against a harsh environment of the gastrointestinal tract. This effectiveness significantly increased by fourfold as compared to free insulin. Taken together, microemulsion seems to be a promising carrier for oral delivery of insulin. |
| Databáze: | OpenAIRE |
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