Drug design, development and therapy, 2018-01, Vol.12, p.1-8
2018
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- Autor(en) / Beteiligte
- Titel
- Development of a nanoliposomal formulation of erlotinib for lung cancer and in vitro/in vivo antitumoral evaluation
- Ist Teil von
- Drug design, development and therapy, 2018-01, Vol.12, p.1-8
- Ort / Verlag
- New Zealand: Dove Medical Press Limited
- Erscheinungsjahr
- 2018
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- The aim of this study was to develop PEGylation liposomes formulations of erlotinib and evaluate their characteristics, stability, and release characteristics. The average particle sizes and entrapment efficiency of PEGylation erlotinib liposomes are 102.4±3.1 nm and 85.3%±1.8%, respectively. Transmission electron microscopy images showed that the liposomes dispersed well with a uniform shape and no changes during the storage. The in vitro drug-release kinetic model of erlotinib release from the PEGylation liposomes in phosphate-buffered saline fit well with the Higuchi equation. In vitro anticancer activity assay showed that the blank liposomes had lower cellular cytotoxicity and that the cellular cytotoxicity of erlotinib liposomes increased significantly under the same incubation condition, which should contribute to the increase in intracellular drug concentration by the transportation of liposomes. The two liposomes of erlotinib (with and without PEGylation) exhibited similar cellular cytotoxicity with no significantly different concentrations. Pharmacokinetic results indicated that erlotinib-loaded PEGylation liposomes can significantly change the pharmacokinetic behavior of drugs and improve the drug bioavailability by nearly 2 times compared to ordinary liposomes. No sign of damages such as the appearance of epithelial necrosis or sloughing of epithelial cells was detected in histological studies.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1177-8881eISSN: 1177-8881DOI: 10.2147/DDDT.S146925Titel-ID: cdi_doaj_primary_oai_doaj_org_article_633299934fbd4cccbb9900ee258cabfe
- Format
- –
- Schlagworte
- A549 Cells, Angiogenesis, Animals, Anticancer properties, Antineoplastic Agents - administration & dosage, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacokinetics, Antitumor activity, Binding sites, Bioavailability, Biocompatibility, Biological Availability, Cancer, Cancer treatment, Care and treatment, cellular cytotoxicity, Chromatography, Cytotoxicity, Dosage and administration, Drug Compounding, Drug delivery systems, Drug dosages, Drug Liberation, Drug Stability, Drug therapy, drug-release, Efficiency, Electron microscopy, Entrapment, Epidermal growth factor, Epithelial cells, Erlotinib, Erlotinib Hydrochloride - administration & dosage, Erlotinib Hydrochloride - chemistry, Erlotinib Hydrochloride - pharmacokinetics, Formulations, Humans, Image transmission, In vivo methods and tests, Incubation, Inhibitor drugs, Injections, Intravenous, Kinases, Lipids, Lipids - chemistry, Liposomes, Lung cancer, Lung Neoplasms - drug therapy, Lung Neoplasms - metabolism, Lung Neoplasms - pathology, Microscopy, Nanomedicine - methods, Nanoparticles, Necrosis, Original Research, Particle Size, PEGyla¬tion liposomal, Pharmacokinetic, Pharmacology, Phosphates, Polyethylene Glycols - chemistry, Protein Kinase Inhibitors - administration & dosage, Protein Kinase Inhibitors - chemistry, Protein Kinase Inhibitors - pharmacokinetics, Rats, Sprague-Dawley, Solubility, Stability analysis, Targeted cancer therapy, Technology, Pharmaceutical - methods, Toxicity, Transmission electron microscopy, Tumors, Xenograft Model Antitumor Assays