Extended release delivery of erlotinib glutathione nanosponge for targeting lung cancer

Abstract

Systemic and uncontrolled administration of erlotinib hydrochloride (ETB) is associated with severe toxicity. A novel targeted and extended release nanosponge (NS) was synthesized from glutathione (GHS) by a one-step reaction between β-cyclodextrin and pyromellitic dianhydride at room temperature for delivery of ETB in lung cancer. Characterization studies were performed using sophisticated instruments. In-vitro release study was performed in the presence of incremental concentrations of GHS which was analyzed using HPLC. Cell cytotoxicity study was evaluated on human lung cancer (A549) cell lines. In-vivo tumour inhibition and biodistribution of ETB-loaded GHS-NS (ETB-NS) were performed on BALB/c mice. NS obtained was spherical, size 212 ± 2.45 nm and high drug entrapment (92.34 ± 5.31%) (p < .001). In-vitro extended drug release (76.89 ± 0.1% release at 168 h), which was directly proportional to the concentration of GHS, demonstrated tumour targeting. There was enhanced in-vitro cytotoxicity and 97.5% inhibition in tumour growth on administering NS when compared to plain ETB (48% inhibition) indicating targeting of NS to the tumour site. Biodistribution study and in-vivo tumour growth inhibition study revealed drug release to the cancerous cell, thus preventing unnecessary drug exposure. ETB-NS exhibits extended drug release proportional to the external GSH concentration.

Comparative Evaluation of Solubility, Cytotoxicity and Photostability Studies of Resveratrol and Oxyresveratrol Loaded Nanosponges

“…Low aqueous solubility of a drug remains a major challenge in order to develop a drug delivery system. Moreover, a rapid drug release is also associated with dose-related toxicity issues [31,32]. In this work, we demonstrated the enhancement in the solubility, photostability, and cytotoxicity of RES and OXY after encapsulation within the CDNSs.…”

Novel therapeutic modalities and drug delivery – erlotinib liposomes modified with galactosylated lipid: in vitro and in vivo investigations

“…As one of commonly used agents for interventional therapy, erlotinib has severe systemic side effects such as skin rash and oedema, which limit its clinical use. This deficiency may be overcome by methods increasing drug accumulation within the tumour or using effective drug carrier that can deliver and release its cargo at the target site [18]. Nevertheless reverse micelle-loaded lipid nanocarriers containing erlotinib hydrochloride were produced by Vrignaud et al [19] recently.…”

A Review on Nanosponges a Review on Nanosponges: A Boon to Targeted Drug Delivery for Anticancer Drug

“…An in-house modified gadget was utilized to check the concentrate penetration of O 2 ; wherein two compartments were isolated using a thin silicon membrane. [97].…”

“…Moreover, the development of drug resistance can further reduce the efficacy of conventional drugs and most molecules are affected by degradation in the gastrointestinal tract. Due to this, the advanced targeted drug delivery systems have gained prime importance in these days [1][2][3][4][5].…”