Determining the Enhancement of Oral Bioavailability VIA Solid Lipid Nanoparticles of Anticancer Drug Dasatinib - An In-vitro Cytotoxicity and Pharmacokinetic Study | Chapter 14 | Current Aspects in Pharmaceutical Research and Development Vol. 2

 Dasatinib (DST) is a Biopharmaceutics Classification System Class II medication with a high permeability and very low solubility. DST's low water solubility and poor dissolution result in low bioavailability. As a result, restricted aqueous solubility represents a bottleneck for DST's therapeutic success. Due to a large first-pass effect, animal research suggests that DST has an absolute bioavailability of 14–34 percent. Lipid-based drug delivery technologies, such as solid lipid nanoparticles (SLNs), can be utilised to circumvent hepatic first-pass metabolism and improve oral bioavailability. Methods: Submicron colloidal carriers with a size range of 50–1000 nm are known as SLNs. These are made from physiological lipids that have been distributed in water or an aqueous surfactant solution. By utilising intestinal lymphatic transport, DST can be easily loaded into SLNs to boost oral bioavailability. In a bioavailability research in rats, an ideal system was compared to that of DST suspension (SUS). Results: ATCC cell lines were used in an in vitro cytotoxicity research using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay technique, the percent inhibition was higher in SLN than in SUS. The pharmacokinetics of DST-SLNs in male Wistar rats following oral administration were investigated. When compared to a DST SUS, DST's bioavailability was improved by 2.28 times. Conclusion: The findings suggest that SLNs are a good lipid-based carrier system for increasing DST oral bioavailability.

Author(s) Details

A. A. Mohamed Yasir Arafath      
Department of Pharmacy Practice, Vinayaka Mission’s College of Pharmacy, Salem, Tamil Nadu, India.

B. Jaykar
Vinayaka Mission’s Research Foundation (Deemed to be University), Salem, Tamil Nadu, India.

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Advanced Study on Preparation, Physical-Chemical Characterization, and Cytocompatibility of Polymeric Calcium Phosphate Cements | Chapter 14 | Current Topics in Medicine and Medical Research Vol. 9

 

Background: Much attention has recently been paid to calcium phosphate cements (CPCs) because of their advantages in terms of in situ handling and forming capabilities compared to calcium phosphate bioceramics. Mechanical and in vitro biological physicochemical properties of novel polymeric calcium phosphate cement (CPC) formulations have been investigated.
Methods: to obtain Forms I, II and III CPCs, monocalcium phosphate, calcium oxide and synthetic hydroxyapatite were mixed either with modified polyacrylic acid, light activated polyalkenoic acid or with polymethyl vinyl ether maleic acid. CPCs were compared with zinc polycarboxylate cement (control) setting time, compressive and diametric strength. X-ray diffraction, scanning electron microscopy, and infrared spectroscopy were used to identify specimens. CPCs and control were tested for in vitro cytotoxicity.
Results: Hydroxyapatite, monetite, and brushite were seen by X-ray diffraction analysis. The presence of stretching peaks in the IR spectra of set cements confirmed the acid-base reaction. Rod-like crystals and platy crystals were disclosed by SEM. The cement setting time was 5-12 min. Compared with power, type III showed significantly higher strength values. High biocompatibility was achieved in type III.
Conclusions: In comparison to zinc polycarboxylate cement (control group), Type III CPC displayed acceptable setting time, substantially higher compressive, and diametral tensile strengths. For dental applications, Type III CPCs show promise.

Author(s) Details


Rania M. Khashaba
Department Oral Biology, Medical College of Georgia, Augusta, GA 30912-1129, USA., Department Orthopaedic Surgery, Section of Biomaterials, Medical College of Georgia, Augusta, GA 30912-1129, USA. and Department of Dental Materials, Misr International University (MIU), Cairo 11787, Egypt.

Mervet Moussa
Department of Oral Pathology, Cairo University, Cairo 11559, Egypt. and Department of Oral Pathology, Misr International University (MIU), Cairo 11787, Egypt.

Christopher Koch
Department Orthopaedic Surgery, Section of Biomaterials, Medical College of Georgia, Augusta, GA 30912-1129, USA.

Arthur R. Jurgensen
Savannah River National Laboratory, Savannah River Nuclear Solutions, Aiken, SC 29808, USA.

David M. Missimer
Savannah River National Laboratory, Savannah River Nuclear Solutions, Aiken, SC 29808, USA.

Ronny L. Rutherford
Savannah River National Laboratory, Savannah River Nuclear Solutions, Aiken, SC 29808, USA.

Norman B. Chutkan
Department Orthopaedic Surgery, Section of Biomaterials, Medical College of Georgia, Augusta, GA 30912-1129, USA.

James L. Borke

Department Oral Biology, Medical College of Georgia, Augusta, GA 30912-1129, USA and Department Orthopaedic Surgery, Section of Biomaterials, Medical College of Georgia, Augusta, GA 30912-1129, USA.

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