Development of a nanoliposomal formulation of erlotinib for lung cancer and in vitro/in vivo antitumoral evaluation

Abstract

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.

Development of Liposomal Vesicles for Osimertinib Delivery to EGFR Mutation—Positive Lung Cancer Cells

“…These properties make TKI potential candidates to be carried by liposomes. TKI can be loaded both in the membrane bilayer via passive loading and in the internal aqueous core by applying active loading; both strategies have yielded clinically useful formulations of other drugs and also have been widely explored to prepare liposomal formulations of other TKIs [ 17 , 18 , 21 , 38 ]. Here, we examined and compared the properties of liposomes loaded with OSI (a new TKI applied in NSCLC) either by a passive or active method.…”

“…Several drug delivery strategies have been previously proposed to enhance the safety and efficacy of TKI-mediated therapy in lung cancer [ 16 , 17 , 18 , 19 , 20 , 21 ]. Liposomes are predominant nanocarriers among these delivery systems that have been developed for TKIs delivery.…”

Multivesicular Liposomes for the Sustained Release of Angiotensin I-Converting Enzyme (ACE) Inhibitory Peptides from Peanuts: Design, Characterization, and In Vitro Evaluation

“…Some dosage forms have been introduced, such as liposomes [11], nanoliposomes [12], nanoparticle suspension [13], oral microemulsion [14,15], and solid dispersions. However, these showed some shortcomings, such as poor long-term stability [16], small drug loading [17], and unobvious release effect.…”

Design, Development and in Vitro Evaluation of Erlotinib Loaded Liquorice Crude Protein Nanoparticles by Box Behnken Design

“…Among the variety of targeting ligands, hyaluronic acid (HA) and human serum albumin have proven success in lung cancer targeting with in tumour cell lines animal models [5]. Moreover a major problem associated with cancer chemotherapy [6,7] is the severe side effects resulting from the normal tissue damage, irrespective of the route of administration, which can be overcome by targeted drug delivery [8,9]. It is aimed to load this drug into a nano drug carrier system, so that it can improve poor solubility and low bioavailability, reduce rapid renal clearance and improve cell selectivity [10,11].…”