phospholipid complex
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2022 ◽  
Vol Volume 17 ◽  
pp. 163-181
Author(s):  
Aya M Khallaf ◽  
Riham M El-Moslemany ◽  
Mahmoud F Ahmed ◽  
Mahmoud H Morsi ◽  
Nawal M Khalafallah

2021 ◽  
Vol 15 ◽  
Author(s):  
Wu-Yan Guo ◽  
Shu-Yan Wang ◽  
Jian Ren ◽  
Bo Zhang

Eurycoma longifolia Jack is a plant of the genus Eurycoma in Simaroubaceae. Eurycomanone is one of the main quassinoids of E. longifolia. Unfortunately, these quassinoids exhibit low bioavailability . In the present study, a phospholipid complex (TAF2-PC) was prepared to improve the oral bioavailability of TAF2 (Tongkat Ali Fraction 2). The complexation rate of eurycomanone and phospholipid was used as the index of success in the phospholipid complexes. The effects of reaction solvent, reaction temperature, drug concentration, drug-lipid ratio and reaction time on thecomplexation rate were investigated. Response Surface-Box-Behnken Design Method was performed to optimize the preparation technology and the pharmacokinetics of phospholipid complex of TAF2 were studied in rats. Our results showed that the optimum preparation condition of TAF2-phospholipid complex were as follows: reaction solvent, anhydrous ethanol; reaction time, 1 h; the ratio of TAF2 to phospholipid, 2.28; reaction temperature, 40.85 ℃; TAF2 concentration, 32.66 mg/ml; and complexation rate, 95.04 ± 0.4% (n=3).The results of pharmacokinetic study showed that the relative bioavailability was increased to 209.20% in the TAF2-phospholipid complex-treated rats.Thus,this phospholipid-complex-technique shows potential for enhancing oral bioavailability of poorly absorbed quassinoid-rich E. longifolia extract, TAF2.


2021 ◽  
Vol 12 (3) ◽  
pp. 3238-3246

An interaction of DNA with lipids is of great interest because of their functions. As fatty acids and lipids can specifically bind to nucleic acids forming a code sequence of the genomic DNA, it is important to study the interaction of the oligonucleotide DNA (dA)20•(dT)20 with phosphatidylglycerol by the molecular dynamics method. Molecular docking has shown that these components form a stable complex with 5.8 kcal/mole binding energy, wherein the lipid is located in the DNA minor groove. This configuration marks 354 atom groups separated by a distance less than 3.4 Ǻ. The van der Waals and hydrophobic interactions play the leading part in the DNA-phospholipid complex stabilization along with hydrogen bonds.


Author(s):  
Shibin Chen ◽  
Qiujie Xie ◽  
Ming Yang ◽  
Yajun Shi ◽  
Junhui Shi ◽  
...  

Background: Baicalin, a flavonoid glycoside compound present in Scutellaria baicalensis, has shown a wide spectrum of biological activities, but its liposolubility, water-solubility and mucosal permeability are all very poor, which lead to the low concentration in brain and poor bioavailability by oral or intravenous injective administration. Objective: The primary objective of this study was to formulate the Scutellaria baicalensis extract (SBE) with phospholipid to yield Scutellaria baicalensis extract-phospholipid complex (SBEPC) and to screen the appropriate administration and dose of SBEPC through the pharmacodynamics experiment. Methods: The optimal preparation process of SBEPC was obtained through single-factor test and central composite design-response surface methodology (CCD-RSM), and was characterized with various analytical techniques including SEM, FT-IR and NMR. The storage conditions of SBEPC were established through stability study and the middle cerebral artery occlusion (MCAO) rat model was investigated through conducting pharmacodynamic studies to screen the appropriate administration and dose of SBEPC as well as to verify the neuroprotective effect of SBEPC on cerebral ischemia-reperfusion injury. Results: The optimized preparation conditions of SBEPC were summarized as follows: the ratio of phospholipids to drug was 2:1, the drug concentration was 3.5 mg/ml, the reaction temperature was 50 °C, the entrapment efficiency was over 93.00%. Stability studies have demonstrated that SBEPC should be stored under 40 °C in a dry and ventilated place away from light and below 37% humidity. Furthermore, pharmacodynamic studies have found that, compared with SBE, SBEPC could introduce drugs into the brain and better exert the neuroprotective effect on MCAO rats, and the optimal administration and dose concentration of SBEPC were nasal administration and 40 mg/ml, respectively. Conclusion: These findings demonstrate that SBEPC was successfully prepared by CCD-RSM. SBEPC can enhance the ability of drugs entering the brain and improve the bioavailability of drugs in brain, and can effectively exert the neuroprotective effect on cerebral ischemia-reperfusion injury as compared with SBE.


2021 ◽  
Vol 22 (5) ◽  
Author(s):  
Ravi Kumar Chakravarti ◽  
Shamandeep Kaur ◽  
Sanjaya K. Samal ◽  
Mahesh C. Kashyap ◽  
Abhay T. Sangamwar
Keyword(s):  

Author(s):  
Waghmare Sagar Saudagar ◽  
GiramPadamja Sidram ◽  
GholveSachin Baburo ◽  
Gaurav Agarwal Shilpi Agarwal ◽  
Bhusnure Omprakash Gadgeppa

Phytosomes are a newly introduced novel drug delivery system and novel botanical formulation to induce lipophilic molecular complexes to enhance absorption and bioavailability of phytoconstituents. Terminali aarjuna phospholipid complex and it’s tablet formulations targeted for cardiovascular systems was prepared. Our study aims is for improving the cardioprotective activity by formulating Terminalia arjuna phospholipid complex tablet by using solvent evaporation method. and characterized by various parameters like solubility studies, particle size determination, infrared absorption (FTIR), Scanning electron microscopy (SEM), entrapment efficiency etc. as well as by applying QbD approach various general characteristics such as entrapment efficiency etc were also done. A QbD- based approach using a Box-Behnken design was done to obtain a response surface design expert software 9.0.5 to systematically study the combined influence of the formulation and process variables such as the phospholipids-drug ratio(X1, w/w), the reaction temperature(X2, °C), and the reaction time (X3, hrs) on a critical quality attributes (CQAs) of the product i.e., the entrapment efficiency. Using this design, the experimental trials were carried out at all 15 possible combinations. The preliminary investigation of the influence of factors revealed that all the tested variables, i.e., the phospholipids to drug ratio, the reaction temperature and the reaction time had a significant influence on the entrapment efficiency of the prepared phytosomes. The study revealed that the entrapment efficiency of Terminalia arjuna Phytosomes was found to be 83.0-97.9 %w/w.


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