Double-loaded liposomes encapsulating Quercetin and Quercetin beta-cyclodextrin complexes: Preparation, characterization and evaluation

Konyak

et al. 2019

Heliyon

Background: Cancer till date remains one of the world's most life threatening disease accompanied by risk of secondary infections. Therefore formulations carrying anticancer drugs which can also decrease the risk of secondary infection are inevitable. Chemotherapeutic drug doxorubicin along with flavonoids quercetin and epigallocatechin gallate (EGCG) is simultaneously loaded on liposomal formulation exploiting the amphiphilic property of the liposomes. Results: Atomic force microscope imaging reveal the size of liposomal formulation loaded with doxorubicin, quercetin and EGCG to be greater than void liposome confirming the presence of drugs. Liposomal stability is improved by PEGylation; adding to the drug release time in vitro. The charge of phosphatidylcholine is rendered positive by coating the formulation with histone. The average size of the formulation is 342 nm. The encapsulation efficiency of doxorubicin, quercetin and EGCG is found to be 65.8%, 96.8% and 98% respectively. The above formulation demonstrated both anticancer and antimicrobial activity. Conclusion: The formulation will provide dual anticancer and antimicrobial therapy thereby evading secondary infection in cancer patients along with chemotherapy.

Section: Resultssupporting

confidence: 93%

Physicochemical characterization of dual action liposomal formulations: anticancer and antimicrobial

Konyak

et al. 2019

Heliyon

J Incl Phenom Macrocycl Chem

“…Liposomes are spherical vesicles with an aqueous core surrounded by lipid bilayers. This unique structure allows liposomes to encapsulate both hydrophilic and lipophilic materials [7]. Currently, liposomes have been extensively investigated for their ability to improve the dissolution properties and release profile of chemotherapeutic agents, in efforts to increase therapeutic efficacy and decrease toxicity to normal cells [8,9].…”

Section: Introductionmentioning

confidence: 99%

Barbigerone-in-hydroxypropyl-β-cyclodextrin-liposomal nanoparticle: preparation, characterization and anti-cancer activities

Qiu

Cai

Wang

et al. 2015

Lipophilic drugs have limited solubility in phospholipid systems, hence maximum entrapment levels in liposomes are known to be low. Barbigerone (Bar), an anticancer isoflavone, is water insoluble and an effective delivery route is through encapsulation in cyclodextrins (CDs) followed by a second encapsulation in liposomes. In this study, Bar or its inclusion complex [Bar/2-hydroxypropyl-b-CD (HP-b-CD)] were incorporated into liposomes prepared by the ethanol injection method. A 4.6-fold increase of encapsulation efficiency was achieved for the liposome-Bar/ HP-b-CD complex (Bar/HP-b-CD/liposome) in comparison with the conventional Bar/liposome. The size of the Bar/HPb-CD/liposome was 87.76 ± 1.45 nm and the zeta potential was -35.02 ± 0.50 mV. In addition, the liposomes remained stable in liquid form at 4°C for at least 3 months. The Bar/HP-b-CD/liposome was evaluated for anti-cancer activity in hepatocarcinoma HepG2 and colon cancer C26 cells and showed comparable toxicity to that of plain Bar. In vivo studies in hepatic cancer xenografted nude mice model showed that Bar/HP-b-CD/liposome significantly inhibited tumor growth with a substantial increase in animal survival. In conclusion, the encapsulation of the Bar/HP-b-CD complex into liposomes could provide an alternative means for its potential use in cancer therapy.

“…The %EE of liposomes varied from 30 to 95%. Significant increase in % EE was observed with increase in cholesterol level but entrapment reduced with the further increase of cholesterol which may be attributed to increasing in rigidity and packing of the membrane and vesicles thus not providing sufficient space for the drug molecules to remain trapped in the lipid layers which in turn reduces the % EE 28 .…”

Section: Results and Discussion: % Ee Size Pdi And Zp Of Liposomesmentioning

confidence: 97%

Untitled

2019

IJPSR

The objective of the study was to formulate coated liposomes containing Prednisolone for colon targeting and localization of the therapy to the inflamed colon mucosa. Liposomes were prepared using thin film hydration method. Liposomal formulations were optimized using 3 2 factorial design using varying concentrations of SPC and cholesterol as independent variables and % EE as the dependent variable. Optimized formulation F5 (60:30) was selected for successive coating with chitosan and eudragit S-100. Chitosan concentration of 1% w/v was taken as optimal based on ZP values. The coated liposomes were encapsulated in eudragit S-100 shell using a solvent-free method. The size if liposomes increased upon addition of the coatings. Fluorescent microscopy aided in clear visualization of chitosan coating around the vesicles. SEM images showed a transition surface appearance in the order smooth-rough-smooth for F5 and the coated liposomes. Eudragit S-100 coated liposomes were subjected to in-vitro drug release studies using simulated fluids for 16 h. ECL5 with 2% w/v eudragit showed sufficient lag time of 6 h. The formulation was able to protect the liposomes in gastric as well as small intestinal conditions, i.e., up to 5 h. Drug release of ECL5 followed zero order kinetics and fitted to Hixon-Crowell release model. The findings of the study conducted indicate a promising approach of the coated liposomes in the targeted release of the drugs.