Comparative Studies on Dissolution and Bioavailability of Tamoxifen Citrate Loaded Binary and Ternary Solid Dispersions
Journal Title: Journal of Pharmaceutical Research International - Year 2014, Vol 4, Issue 2
Abstract
Aims: This study focused on comparing binary and ternary solid dispersions (SD's) of water-insoluble Tamoxifen citrate (TMC) regarding drug dissolution and oral bioavailability. Basically, the enhanced dissolution of this drug by water-soluble polymer has not yet been reported in literature. Study Design: In vitro and In-vivo characterization of Tamoxifen citrate loaded binary and ternary solid dispersion systems. Place and Duration of Study: Department of Pharmaceutics and Industrial Pharmacy, Helwan University, Cairo, Egypt between June 2012 and June 2013. Methodology: Amorphous SD's of TMC with two hydrophilic polymers, polyethylene glycol 6000 (PEG 6000) and Methyl cellulose (MC), were prepared by melting method. Binary SD's of TMC with PEG of different weight ratios were prepared. MC was used as third component to prepare ternary SD's. Physicochemical properties of SD's were characterized by FTIR, DSC, and In-vitro drug release in comparison with physical mixtures and the drug alone. Oral bioavailability of the optimized SD formula was compared with that of free TMC in rats. Results: Infrared spectroscopic studies suggested no interaction between TMC and polymers rather than H-bond formation. A remarkably improved dissolution of drug from the ternary solid dispersion systems when compared to the binary solid dispersion systems was detected. On the basis of % dissolution efficiency (% DE), the SD composed of PEG: TMC: MC in a ratio 4:1:2 w/w/w was selected as the optimized SD. The in-vivo studies showed extremely significant higher values of Cmax (P<.05), AUC0-24 (P<.05) and significantly (P<.05) lower values of Tmax exhibited by SD compared with free TMC. Conclusion: Highly enhanced TMC dissolution and bioavailability exhibited by PEG: TMC: MC ternary solid dispersion in a weight ratio 4:1:2 were promising to improve the therapeutic potential of TMC.
Authors and Affiliations
Dalia S. Shaker, Mohamed K. Ghorab, Mohamed S. Teiama
Keywords
Related Articles
- EP ID EP344307
- DOI 10.9734/BJPR/2014/6072
- Views 92
- Downloads 0
“The Nutraceutical Amino Acids”- Nature’s Fortification for Robust Health
Nutraceuticals i.e. the product positioned at the interface between food and drugs, are an increasing group of products gaining importance; patients/consumers of drug always have a wish to have no or less side/ toxic eff...
Phytochemical and Antibacterial Studies on Aqueous Ethanol Extract of Thesium viride (Santalaceae)
Thesium viride Hill (Santalaceae) is a sub-shrub hemiparasite that grows up to 45 cm tall and widely distributed in Europe, Asia and Africa. It is used ethno medicinally in ulcer, jaundice and splenomegally. Phytochemica...
Formulation and Characterization of Nystatin-loaded Nanostructured Lipid Carriers for Topical Delivery against Cutaneous Candidiasis
Aims: The objective of the current study was to formulate nystatin (Nyst) into nanostructured lipid carriers (NLCs) to enhance its antifungal activity. Place and Duration of Study: Department of pharmaceutical technolog...
Investigation of Design Principles and Users Demand for Hospital Gardens: Case Study of Egirdir-Turkey
Aims: The plants in hospital garden have many functions to users. Hence attention on those areas should be done. A specific hospital and its gardens chosen to be determine expectations and express of users to determine s...
X-ray Crystal Structure of COX-2 Enzyme as a Tool to Predict Active Sites of Bitter Taste Receptors
This commentary discusses a novel approach to be used in the design of active sites of bitter taste receptors, especially TAS2R14, by using the X-ray crystal structure of the enzyme COX-2 and chemical structures of commo...