Gefitinib loaded nanostructured lipid carriers: characterization, evaluation and anti-human colon cancer activity in vitro

Abstract

NLC containing Gefitinib (NANOGEF) was prepared using stearic acid, sesame oil and surfactants (sodium lauryl sulfate and tween 80). NANOGEFs were evaluated for particle size, polydispersity index (PdI), zeta potential, entrapment efficiency (EE), stability, release studies and cytotoxicity studies (MTT assay). The optimized NANOGEF exhibited particle size of 74.06 ± 9.73 d.nm, PdI of 0.339 ± 0.029 and EE of 99.76 ± 0.015%. The TEM study revealed spherical shape of NANOGEF formulations. The slow and sustained release behavior was exhibited by all NANOGEFs. The effects of surfactants were observed not only on particle size but also on zeta potential, entrapment efficiency, stability and release studies. The MTT assay revealed 4.5 times increase in cytotoxicity for optimized NANOGEF (IC 50 ¼ 4.642 mM) when compared with Gefitinib alone (IC 50 ¼ 20.88 mM in HCT-116 cells). Thus NANOGEF may be considered as a potential drug delivery system for the cure of colon cancer.

Preparation, Characterization and Anti-cancer Activity of Nanostructured Lipid Carriers Containing Imatinib

“…NANIMA was prepared using the fat and oil by hot homogenization method [9]. Moreover, the surfactants including SLS and T80 were used for the stabilization of the system.…”

“…Hence, amid the fatty acid chains and/or lipid layers the IMA molecules can be accommodated in higher amount. Moreover, the parallel outcomes were perceived previously [9,28,29,30,31].…”

“…Furthermore, the benefits associated with the particular properties of lipid nanocarriers include tumor-specific drug deposition, efficient pharmacokinetics and pharmacodynamics account of therapeutic agent, enhanced internalization and intracellular transport , and decreased biodistribution, resulting in the mitigation of harmful consequences of anti-tumor treatments [7,8]. The administration of various drug molecules such as gefitinib [9], celecoxib [10], doxorubicin [11], duloxetine [12], tamoxifen [13], curcumin [14], and paclitaxel [15] has been extensively investigated using nanostructured lipid carriers (NLC). Because of their fast intake by cells, biodegradability, and bio-acceptability [9], NLCs are being studied extensively for drug delivery.…”

“…The administration of various drug molecules such as gefitinib [9], celecoxib [10], doxorubicin [11], duloxetine [12], tamoxifen [13], curcumin [14], and paclitaxel [15] has been extensively investigated using nanostructured lipid carriers (NLC). Because of their fast intake by cells, biodegradability, and bio-acceptability [9], NLCs are being studied extensively for drug delivery. It has better controlled release features and drug loading capability, as well as a lower burst release rate [16].…”

Light-Responsive Micelles Loaded With Doxorubicin for Osteosarcoma Suppression

“…The nano-carrier can achieve the controllable sustained release of various chemotherapeutic drugs in the drug delivery environment according to the design needs so that the active molecules form a highly dominant concentration in the local tumor and effectively kill tumor cells (Hanafy et al, 2018). Moreover, it substantially avoids the whole-body distribution of biotoxic molecules and effectively avoids all kinds of toxic and side effects of traditional chemotherapy drug delivery, so it is the most appropriate dosage form for carrying anticancer drugs (De Vos et al, 2014;Pradeep et al, 2017;Makeen et al, 2020). Nanomicelles have achieved great success in the current cell and animal experiments, but due to the defects that the drug is released ahead of time and the drug carrier cannot fully release the drug when it reaches the focus, the clinical application of drug-loaded micelles is limited (Sethuraman et al, 2021).…”