Assessment of Aprotinin Loaded Microemulsion Formulations for Parenteral Drug Delivery: Preparation, Characterization, in vitro Release and Cytotoxicity Studies
| Autor: | Zeynep Ay Şenyiğit, Derya İlem Özdemir, Makbule Asikoglu, Lütfi Genç, H. Yeşim Karasulu, Şennur Görgülü Kahyaoğlu, Neslihan Üstündağ Okur |
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| Přispěvatelé: | Anadolu Üniversitesi, Bitki, İlaç ve Bilimsel Araştırmalar Merkezi, Genç, Lütfi |
| Rok vydání: | 2015 |
| Předmět: |
In Vitro Release
Cytotoxicity Chemistry Pharmaceutical Drug Compounding Drug Storage Pharmaceutical Science Tc-99m-Aprotinin Aprotinin Drug Delivery Systems Drug Stability Zeta potential medicine Humans Microemulsion Particle Size Cells Cultured Chromatography Chemistry Viscosity Pancreatic Ducts Technetium Epithelial Cells In vitro Drug Liberation Pancreatitis Drug delivery Chemical stability Emulsions Particle size Trypsin Inhibitors hormones hormone substitutes and hormone antagonists medicine.drug |
| Zdroj: | Current drug delivery. 12(6) |
| ISSN: | 1875-5704 |
| Popis: | WOS: 000372334800004 PubMed ID: 26306401 The object of the current study was to prepare novel microemulsion formulations of aprotinin for parenteral delivery and to compare in vitro characteristics and release behaviour of different Technetium-99m (Tc-99m)-Aprotinin loaded microemulsion formulations. In addition, cytotoxicity of microemulsion formulation was evaluated with cell culture studies on human immortalized pancreatic duct epithelial-like cells. For this aim, firstly, pseudo-ternary phase diagrams were plotted to detect the formulation region and optimal microemulsions were characterized for their thermodynamic stability, conductivity, particle size, zeta potential, viscosity, pH and in vitro release properties. For in vitro release studies aprotinin was labelled with Tc-99m and labelling efficiency, radiochemical purity and stability of the radiolabeled complex were determined by several chromatography techniques. Radiolabeling efficiency of Tc-99m-Aprotinin was found over than 90% without any significant changes up to 6 hours after labelling at room temperature. After that, in vitro release studies of Tc-99m-Aprotinin loaded microemulsions were performed with two different methods; dissolution from diffusion cells and dialysis bags. Both methods showed that release rate of Tc-99m-Aprotinin from microemulsion could be controlled by microemulsion formulations. Drug release from the optimized microemulsion formulations was found lower compared to drug solution at the end of six hours. According to stability studies, the optimized formulation was found to be stable over a period of 12 months. Also, human immortalized pancreatic duct epithelial-like cells were used to evaluate the cytotoxicity of optimum formulation. Developed microemulsion did not reveal cytotoxicity. In conclusion the present study indicated that the M1-APT microemulsion is appropriate for intravenous application of aprotinin. Scientific and Technological Research Council of Turkey [Tubitak-108S083] This study was supported by The Scientific and Technological Research Council of Turkey (Tubitak-108S083). We would like to acknowledge Ege University Pharmaceutical Sciences Research Center (FABAL) for enabling us to use its laboratory instruments. The authors would like to thank to Ege University, Faculty of Pharmacy, and Department of Microbiology. The authors would like to thank Ismail Ozturk for assistance at sterility experiments. |
| Databáze: | OpenAIRE |
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