Quercetin loaded targeted liposome formulation used for breast cancer, comprises quercetin, lipid, cholesterol, and folate-labeled DSPE-PEG comprising folic acid, dimethyl sulfoxide, dicyclohexylcarbodiimide, pyridine and N-(aminopropylpolyethyleneglycolcalbamyl) stearoylphosphatidyl ethanol amine
	YAMINI B; PETHANI T; RAVIRAJ B; PATEL P
	2023-09-20
专利权人	YAMINI B (YAMI-Individual) ; PETHANI T (PETH-Individual) ; RAVIRAJ B (RAVI-Individual) ; PATEL P (PATE-Individual) ; UNIV SAURASHTRA (UYSA-Non-standard)
申请日期	2023-09-20
专利号	IN202321063161-A
成果简介	NOVELTY - Quercetin loaded targeted liposome formulation comprises: quercetin, lipid, cholesterol, surfactant, organic solvent, phosphate buffer pH 7.4 and folate-labeled 1, 2-Distearoyl-sn-glycero-3-phosphoethanolamine-Poly(ethylene glycol) (DSPE-PEG) as active targeting agent, where active targeting agent comprising folic acid, dimethyl sulfoxide, dicyclohexylcarbodiimide, pyridine, N- (aminopropylpolyethyleneglycolcalbamyl) stearoylphosphatidyl ethanol amine. USE - Quercetin loaded targeted liposome formulation used for treatment of breast cancer. ADVANTAGE - The formulation is safe, biocompatible, and effective with less side effects; provide prolong drug release; increase efficacy and therapeutic index; low therapeutic doses; and improve oral bioavailability, and patient compliance. The pharmacokinetic profile of the formulation was tested in rat plasma. The results showed that formulation comprising 10 mg quercetin, 100 mg lipid, 75 mg cholesterol, 10 mg surfactant, 25 mL organic solvent, 40 mL phosphate buffer pH 7.4 and 12.5 mg folate-labeled PEG-DSPE exhibited an Cmax of 772 ng/mL. DETAILED DESCRIPTION - An INDEPENDENT CLAIM is included for a process of preparation of quercetin loaded targeted liposome formulation, which involves: (a) weighing soya lecithin, poloxamer 188, cholesterol, folate-labeled PEG-DSPE and quercetin properly; (b) dissolving step (a) into chloroform and mixing; (c) removing chloroform solvent by using rotary evaporator under vacuum; (d) hydrating lipid layer from step (c) with phosphate buffer solution (PBS) (pH 7.4); (e) sonicating the suspension by using probe sonication for 15 minutes, and then homogenizing for 5 minutes to get multilamellar vesicles of various size; (f) passing liposome from step (e) into lypex extruder with 200 nanometers (nm) membrane filter; (g) storing suspension from step (f) for 24 hours at 2℃ in refrigerator; (h) removing unentrapped drug from liposome dispersions by centrifugation at 12000 rotation/minute (rpm) for 20 minutes; (i) resuspending liposome pellets into phosphate butter solution; (j) lyophilizing the solution in vials in lyophilizer by cooling the solution down to -44℃ for 2 hours for lyophilization cycle, then primary drying for 48 hours at -32℃, temperature from (-)32-(-)5℃ for 24 hours, and second drying at 24℃ for 8 hours; and (k) collecting lyophilized folate conjugate liposome and storing.
IPC 分类号	A23L-033/105 ; A61K-031/352 ; A61K-047/36 ; A61K-008/02 ; A61K-008/49 ; A61K-008/73 ; A61K-009/14 ; A61P-035/00
国家	印度
专业领域	医药卫生
语种	英语
成果类型	专利
文献类型	科技成果
条目标识符	http://119.78.100.226:8889/handle/3KE4DYBR/20308
专题	中国科学院新疆生态与地理研究所
作者单位	1.YAMINI B (YAMI-Individual) 2.PETHANI T (PETH-Individual) 3.RAVIRAJ B (RAVI-Individual) 4.PATEL P (PATE-Individual) 5.UNIV SAURASHTRA (UYSA-Non-standard)
推荐引用方式 GB/T 7714	YAMINI B,PETHANI T,RAVIRAJ B,et al. Quercetin loaded targeted liposome formulation used for breast cancer, comprises quercetin, lipid, cholesterol, and folate-labeled DSPE-PEG comprising folic acid, dimethyl sulfoxide, dicyclohexylcarbodiimide, pyridine and N-(aminopropylpolyethyleneglycolcalbamyl) stearoylphosphatidyl ethanol amine. IN202321063161-A[P]. 2023.

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