Comparative Studies on Dissolution and Bioavailability of Tamoxifen Citrate Loaded Binary and Ternary Solid Dispersions

Shaker, Dalia S.

doi:10.9734/bjpr/2014/6072

Cited by 4 publications

(3 citation statements)

References 26 publications

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“…Our findings agree with a previously reported T max of 4 to 7 hours for free TC [27]. Past work has shown that the elimination of TC is biphasic with a first-phase half-life of 7 hours and a terminal half-life of 7-11 days [28–30]. As a result, TC has two values of elimination rate constant, K at 0.098 h-1 487 (initial half-life) and 0.004 h-1 381 (terminal half-life).…”

Section: Resultssupporting

confidence: 93%

An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

Sreeharsha

Hiremath²,

Chilukuri

et al. 2019

BioMed Research International

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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.

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Section: Resultssupporting

confidence: 93%

An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

Sreeharsha

Hiremath²,

Chilukuri

et al. 2019

BioMed Research International

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“…The DSC thermogram of pure TMC showed a sharp endothermic peak at 145.8 °C (figure 3, C) corresponding to its melting point and indicating the crystalline nature of TMC with enthalpy fusion ∆H= 39.95 J/g(Shaker et al, 2014). The thermal analysis of Span 60 surfactant showed an endothermic peak at its melting point 59.32 °C with enthalpy fusion ∆H= 155.88 J/g (figure 4, A), whereas cholesterol showed also an endothermic peak at 51.56 °C with enthalpy fusion ∆H= 48.28 J/g (figure 3, B).…”

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confidence: 99%

Cellular uptake, cytotoxicity and in-vivo evaluation of Tamoxifen citrate loaded niosomes

Shaker

Hanafy

2015

International Journal of Pharmaceutics

112

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“…Significant amount of research has been published to improve the bioavailability of Tamoxifen citrate by addition of cyclodextrin or solubility enhancers (Allan et al, 1985). Tamoxifen citrate loaded ternary solid dispersion was prepared using PEG 6000 and Methyl cellulose to enhance its bioavailability and solubility (Shaker, 2014). Through this type of formulations, not only the solubility of Tamoxifen citrate is enhanced but the side effect is also diminished.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Development of Transferrin Targeted Solid Lipid Nanoparticles for Breast Cancer Therapy

et al. 2020

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Breast cancer is conventionally treated by surgery, chemotherapy and radiation therapy followed by post operational hormonal therapy. Tamoxifen citrate is a best option to treat breast cancer because its selective estrogen receptor modulation activity. Owing to its antiestrogenic action on breast as well as uterine cells, Tamoxifen citrate shows uterine toxicity. The dose 20 mg per day of Tamoxifen citrate required to show therapeutic effect causes side effects and toxicity to vital organs such as liver, kidney and uterus. In the present study, transferrin-conjugated solid lipid nanoparticles (SLNs) were successfully prepared to enhance the active targeting of tamoxifen citrate in breast cancer. Developed formulations were evaluated for particle size, surface charge, surface morphology and in vitro dissolution studies. Developed formulations exhibited more cytotoxicity as compared to pure Tamoxifen citrate solution in time as well as concentration dependent manner on human breast cancer MCF-7 cells. Further, cell uptake and flow cytometry studies confirmed the qualitative uptake of developed D-SLN and SMD-SLN by human breast cancer MCF-7 cells. Overall, proposed study highlights that transferrin engineered nanocarriers could enhance the therapeutic response of nanomedicines for breast cancer treatment.

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Comparative Studies on Dissolution and Bioavailability of Tamoxifen Citrate Loaded Binary and Ternary Solid Dispersions

Abstract: MKG managed the analyses of the study. Author MST managed the literature searches. Author MST run experiments and performed the statistical analysis. All authors read and approved the final manuscript.

Cited by 4 publications

References 26 publications

An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

Cellular uptake, cytotoxicity and in-vivo evaluation of Tamoxifen citrate loaded niosomes

Formulation and Development of Transferrin Targeted Solid Lipid Nanoparticles for Breast Cancer Therapy

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