Development of biodegradable polymer based tamoxifen citrate loaded nanoparticles and effect of some manufacturing process parameters on them: a physicochemical and in-vitro evaluation

Abstract

Abstract:The aim of the present study was to develop nanoparticles of tamoxifen citrate, a non-steroidal antiestrogenic drug used for the treatment of breast cancer. Biodegradable poly (D, L-lactide-co-glycolide)-85:15 (PLGA) was used to develop nanoparticles of tamoxifen citrate by multiple emulsification (w/o/w) and solvent evaporation technique. Drug-polymer ratio, polyvinyl alcohol concentrations, and homogenizing speeds were varied at different stages of preparation to optimize the desired size and release profile of drug. The characterization of particle morphology and shape was performed by field emission scanning electron microscope (FE-SEM) and particle size distribution patterns were studied by direct light scattering method using zeta sizer. In vitro drug release study showed that release profile of tamoxifen from biodegradable nanoparticles varied due to the change in speed of centrifugation for separation. Drug loading efficiency varied from 18.60% to 71.98%. The FE-SEM study showed that biodegradable nanoparticles were smooth and spherical in shape. The stability studies of tamoxifen citrate in the experimental nanoparticles showed the structural integrity of tamoxifen citrate in PLGA nanoparticles up to 60°C in the tested temperatures. Nanoparticles containing tamoxifen citrate could be useful for the controlled delivery of the drug for a prolonged period.

Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain

“…FTIR was conducted to determine possible interaction (if any) between the drug and the excipients. For ML-based formulation, pure drug (AZT), CHO, ML, BHT, physical mixture (PM) of CHO, ML, BHT, physical mixture (PMD) of CHO, ML, BHT and drug AZT, lyophilized formulation without drug (MGB) and lyophilized formulation with drug (MGF) and for SL-based formulation, AZT, CHO, SL, BHT, physical mixture (PM-1) of CHO, SL, BHT, physical mixture (PMD-1) of CHO, SL, BHT and AZT, lyophilized formulation without drug (SYB) and lyophilized formulation with drug (SYF) were scanned at 4000–400 cm −1 using FTIR instrument (JASCO International Co. Ltd., FTIR 4200, Tokyo, Japan) using their pellets formed by mixing with potassium bromide (KBr) at 1:100 ratio and compressing with a hydraulic press (Sahana et al., 2010 ).…”

“…To determine the yield of NLs from the utilized total amount of raw materials of NLs preparation, lyophilized dried NLs of each batch were weighed and the percentage of yield was calculated by using the following equation as mentioned earlier (Sahana et al., 2010 ). …”

“…Stability testing of the lyophilized formulations was performed as per ICH guidelines (Sahana et al., 2010 ).…”

Lipid-drug conjugates: a potential nanocarrier system for oral drug delivery applications

“…For instance, many studies have been performed and showed spherical shaped nanoparticles [22, 26, 32, 33]. Field emission SEM (FE-SEM) is more sensitive than SEM as it allows detecting samples within nanometer range [34].…”

Layer-by-Layer Nanoparticles of Tamoxifen and Resveratrol for Dual Drug Delivery System and Potential Triple-Negative Breast Cancer Treatment

“…Tamoxifen citrate (TAM) is commonly employed as a non-steroidal estrogen antagonist in ER+ breast cancer therapeutics, in addition to long-term preventive use in risky and post-menopausal women [ 19 ]. TAM acts by causing apoptosis through cell-cycle arrest [ 20 ]; it also acts as an anti-oxidant [ 21 ] and may stimulate tumoricidal effects on ER-cells through increased inhibitory growth factor production [ 22 ]. Although promising, TAM is eliminated via hepatic first-pass metabolism with a detectable drug concentration up to 24 h of oral administration [ 23 ].…”