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An Approach to Enhance Dissolution Rate of Tamoxifen Citrate.
Biomed Res Int. 2019; 2019:2161348.BR

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.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.Department of Pharmaceutics, Oxbridge College of Pharmacy, Herohalli Cross, Magadi Road, Bangalore, India.Department of Pharmaceutics, East West College of Pharmacy, Bangalore-560 091, Karnataka, India.Hetero Drugs Ltd, 7-2-A2, Hetero Corporate, Industrial Estates, Sanath Nagar, Hyderabad-500 018. Telangana, India.Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia. Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa.Department of Biological Sciences, College of Science, King Faisal University, Al-Ahsa, Saudi Arabia.Department of Biomedical Sciences, College of Medicine, King Faisal University, Al-Ahsa, Saudi Arabia.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30800663

Citation

SreeHarsha, Nagaraja, et al. "An Approach to Enhance Dissolution Rate of Tamoxifen Citrate." BioMed Research International, vol. 2019, 2019, p. 2161348.
SreeHarsha N, Hiremath JG, Chilukuri S, et al. An Approach to Enhance Dissolution Rate of Tamoxifen Citrate. Biomed Res Int. 2019;2019:2161348.
SreeHarsha, N., Hiremath, J. G., Chilukuri, S., Aitha, R. K., Al-Dhubiab, B. E., Venugopala, K. N., Alzahrani, A. M., & Meravanige, G. (2019). An Approach to Enhance Dissolution Rate of Tamoxifen Citrate. BioMed Research International, 2019, 2161348. https://doi.org/10.1155/2019/2161348
SreeHarsha N, et al. An Approach to Enhance Dissolution Rate of Tamoxifen Citrate. Biomed Res Int. 2019;2019:2161348. PubMed PMID: 30800663.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - An Approach to Enhance Dissolution Rate of Tamoxifen Citrate. AU - SreeHarsha,Nagaraja, AU - Hiremath,Jagadeesh G, AU - Chilukuri,Swathi, AU - Aitha,Rajesh Kumar, AU - Al-Dhubiab,Bandar E, AU - Venugopala,Katharigatta N, AU - Alzahrani,Abdullah Mossa, AU - Meravanige,Girish, Y1 - 2019/01/20/ PY - 2018/10/14/received PY - 2018/11/04/revised PY - 2018/12/10/accepted PY - 2019/2/26/entrez PY - 2019/2/26/pubmed PY - 2019/6/14/medline SP - 2161348 EP - 2161348 JF - BioMed research international JO - Biomed Res Int VL - 2019 N2 - 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. SN - 2314-6141 UR - https://www.unboundmedicine.com/medline/citation/30800663/An_Approach_to_Enhance_Dissolution_Rate_of_Tamoxifen_Citrate_ L2 - https://doi.org/10.1155/2019/2161348 DB - PRIME DP - Unbound Medicine ER -