An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

Abstract

We tested the solubility and dissolution of tamoxifen citrate to ascertain the optimal conditions for faster dissolution. Using the solvent evaporation method and hydrophilic carriers, we formulated tamoxifen citrate (TC) that contained solid dispersions (SDs). We increased the solubility and dissolution rate of TC with a solid dispersion system that consisted of polyethylene glycol (PEG-6000), beta-cyclodextrin (β-CD), and a combination of carriers. Physicochemical characteristics of solubility (mg/ml) were found to be 0.987±0.04 (water), 1.324±0.05 (6.8pH PBS), and 1.156±0.03 (7.4 pH PBS) for F5 formulation, percentage yield was between 98.74 ± 1.11% and 99.06 ± 0.58%, drug content was between 98.06±0.58 and 99.06±1.10, and dissolution studies binary complex showed a faster release of TC as compared to a single polymer and pure drug. Furthermore, thermal properties, physicochemical drug and polymer interaction, crystal properties, and morphology were determined using differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), X-ray differential studies, and scanning electron microscopy. We used the same proportion of carrier concentrations of the formulations to calculate the solubility of TC. Our results demonstrated that increased concentrations of β-C yielded an improved solubility of TC, which was two times higher than pure TC. The uniformity in drug content was 97.99 %. A quicker drug release occurred from the binary complex formulation as seen in the dissolution profile. FTIR demonstrated an absence in the physicochemical interaction between the drug and carriers. The drug was also found to be dispersed in the amorphous state as revealed by DSC and XRD. The drug concentration did not vary during various storage conditions. Our in vivo studies demonstrated that SD displayed significantly higher values of Cmax (p < 0.05) and AUC0-24 (p < 0.05) as compared to free TC. Furthermore, Tmax in SD was significantly lower (p < 0.05), as compared to free TC.

Solid Self-Nano Emulsifying Nanoplatform Loaded with Tamoxifen and Resveratrol for Treatment of Breast Cancer

“…The DSC curve of TAM and RES (Figure 6a) showed a sharp endothermic peak (the point where the substance absorbs the heat, reaching its melting point, and changes from a crystalline to amorphous form) at 147.721 • C and 266.919 • C, which is same as reported in the literature [78,79]. The DSC curve of the mixture of both drugs (Figure 6a) also showed the same endothermic peaks with a slight shift in the height, shape and positions of the peaks due to the difference in the geometry of the mixture [80].…”

Paclitaxel loaded poly (DL lactic acid co castor oil) 60:40 with poloxamer‐F68 rod shape cylindrical nanoparticle preparation and in vitro cytotoxicity studies

“…Page and Dupont define breast cancer as a familiar or atypical ductal hyperplasia or lobular hyperplasia, having in situ cancer. It relates functional and genetic alterations expressed at the molecular level correlated with these anatomical changes causes of breast cancer or cancer . Breast cancer is the most occurring malignant disease in young women in growing countries, leading to the greatest estimate of early deaths.…”

“…It relates functional and genetic alterations expressed at the molecular level correlated with these anatomical changes causes of breast cancer or cancer. 2,3 Breast cancer is the most occurring malignant disease in young women in growing countries, leading to the greatest estimate of early deaths. The breast cancer mortality rate has decreased because of the need of country limited, population-based mammography screening.…”

Enantioselective Resolution of (R, S)-DMPM by a Adsorption-Covalent Crosslinked Esterase PAE07 from Pseudochrobactrum Asaccharolyticum WZZ003

“…Therefore, the enzyme activity of immobilized esterase PAE07 was inhibited under both low and high concentration of enzyme loading. This is because under a high concentration of enzyme loading, the resin will produce multi-layer adsorption of the enzyme, so that the resin does not have enough speci c surface to bind with the enzyme, and it may also block the pores of the resin and affect the binding of the esterase and the substrate [29,30]. Conversely, at low concentrations of enzyme loading, the esterase will try to maximize contact with the resin surface, resulting in loss of conformation and inactivation [31].…”