Raloxifene-loaded solid lipid nanoparticles decorated gel with enhanced treatment potential of osteoporosis was written by Guo, Zhonghua;Qi, Ping;Pei, Donghong;Zhang, Xiuju. And the article was included in Journal of Drug Delivery Science and Technology in 2022.Formula: C21H44O5 The following contents are mentioned in the article:
Osteoporosis is a common metabolic disorder associated with global morbidities and mortalities which make it a big challenge to the public health. Despite the availability of a number of drugs, its treatment is challenging due the drugs associated complications including poor dissolution, abridged permeation, reduced bioavailability and severe toxicities. This study aims to develop Raloxifene HCl-loaded solid lipid nanoparticles (RAL-SLNs) decorated gel in order to address the above-mentioned problems. RAL-SLNs were prepared by high pressure homogenization and evaluated in terms of their size distribution, morphol., zeta potential and drug entrapment using DLS anal., TEM and HPLC. Prior to this, screening of the lipid and surfactant was done based on drug solubility ratio. The optimized SLNs were further incorporated in chitosan gel to develop RAL-SLNs decorated gel (RAL-SLNsG) and were characterized in terms of their rheol. properties, pH and spreadability. In vitro drug release, kinetics of drug release and permeation analyses of the RAL-SLNsG were performed and compared with drug suspension and RAL gel (conventional gel) to check the release and permeation ability of the incorporated dug. Moreover, pharmacokinetics study of the test formulations was performed to check the bioavailability. Addnl., biochem. estimation was done after inducing osteoporosis in rats and their treatment with RAL-SLNsG and RAL gel after transdermal administration and were compared with pos. and neg. control groups. RAL-SLNs were found to have rounded shaped size distribution of 170 nm with -24.5 mV zeta potential and 95% drug entrapment. The RAL-SLNsG has excellent spreadability, optimum and non-Newtonian flow behavior. In vitro release and ex vivo permeation showed 7-fold and 11-fold enhanced properties, as compared to RAL suspension, resp. Bioavailability study revealed 3-fold and 6-fold enhanced bioavailability of the drug when incorporated in SLNs decorated gel as compared to the conventional gel and drug suspension. Finally, the serum level of alk. phosphatase and calcium were found to be significantly reduced in osteoporosis induced rats after treatment with RAL-SLNsG decorated gel as compared to RAL gel. These finding revealed that nanogel has the potential to enhance the permeation and bioavailability of incorporated drug with enhanced anti-osteoporotic effect. This study involved multiple reactions and reactants, such as Glyceryl monostearate (cas: 31566-31-1Formula: C21H44O5).
Glyceryl monostearate (cas: 31566-31-1) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Formula: C21H44O5
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics