Development of chitosan-based dry powder inhalation system of cisplatin for lung cancer

Abstract

Cisplatin, a platinum compound, exerts its cytotoxic effects by coordinating to DNA where it inhibits both replication and transcription, and induces programmed cell death. It is used in the treatment of non-small cell lung cancer. In the present study, an attempt was made to achieve better treatment of lung cancer by direct lung delivery of cisplatin microparticulate systems, which helps to localize the drug in the lungs, and also provide sustained action. Cisplatin-loaded chitosan microspheres were prepared by emulsification and ionotropic gelation method, and characterized for drug content, particle size, densities, flow properties, moisture content, and surface topography by SEM and in vitro drug release was evaluated in simulated lung fluid at 37° at pH 7.4. The respirable or fine particle fraction (FPF) was determined by using twin stage impinger (TSI). Further stability evaluation of cisplatin-loaded DPI systems was carried out at 25°/60% RH and at 40°/75% RH.

Electrochemical Deposition of Cisplatin on Pure Magnesium

“…D. J. Singh et al 25 prepared cisplatin-loaded chitosan microspheres by emulsification and ionotropic gelation method. The drugs content was 79.2 ± 2.9% and the mean particle size was 5.2 ± 1.19 μm.…”

Stability of Chitosan—A Challenge for Pharmaceutical and Biomedical Applications

“…Chitosan co-crystals with acyclovir prepared by a solvent change method using sodium citrate as the salting out compound exhibited good physical stability with regard to the drug content and drug release profile upon three-month storage at 40 °C/75% RH [ 110 ]. Singh et al, studied the long-term stability of cisplatin-loaded chitosan glutamate microparticles, crosslinked with citric acid prepared by emulsification-ionotropic gelation [ 28 ]. No significant changes in physical appearance and drug content in all formulations stored in high-density polyethylene containers at 40 °C/75% RH and 25 °C/60% RH upon correspondingly 6- and 12-month periods were noticed.…”

“…No significant changes in physical appearance and drug content in all formulations stored in high-density polyethylene containers at 40 °C/75% RH and 25 °C/60% RH upon correspondingly 6- and 12-month periods were noticed. However, an approximately 17%–19% increase in moisture content and subsequent rise in the particle size during both long-term and accelerated stability studies were observed suggesting that chitosan microparticles might be still susceptible to physicochemical degradation over time [ 28 ].…”

A review on chitosan and its development as pulmonary particulate anti-infective and anti-cancer drug carriers

“… Nil The microspheres are characterised by a higher IC 50 value when compared to free drug due to a slower drug release from the matrix thus negating the drug bioavailability. ( Menon et al, 2012 ) F4 Raloxifene loaded hyaluronic acid and chitosan nanoparticles are prepared by single emulsion solvent evaporation method. The nanoparticles are constituted of a core and surrounded by multilayers of hyaluronic acid- and chitosan-based shell.…”