PEGylated Lipova E120 liposomes loaded with celecoxib: in-vitro characterization and enhanced in-vivo anti-inflammatory effects in rat models

Brown adipose tissue (BAT) is responsible for adaptive thermogenesis. We previously showed that genetic deficiency ofreceptor for advanced glycation end products (RAGE) prevented the effects of high-fat diet (HFD). This study was tocompare BAT activity in RAGE knock out (Ager-/-, RKO) and wild-type (WT) mice after treated with HFD or LFD.[18F]FDG PET-CT imaging under identical cold-stimulated conditions and mean standard uptake values (SUVmean), ratio ofSUViBAT/SUVmuscle (SUVR, muscle as the reference region) and %ID/g were used for BAT quantification. The resultsshowed that [18F]FDG uptake (e.g., SUVR) in WT-HFD mice was significantly reduced (three-fold) as compared to that inWT-LFD (1.40 ± 0.07 and 4.03 ± 0.38; P = 0.004). In contrast, BAT activity in RKO mice was not significantly affectedby HFD, with SUVRRKO-LFD: 2.14 ± 0.10 and SUVRRKO-LFD: 1.52 ± 0.13 (P = 0.3). The uptake in WT-LFD was almostdouble of that in RKO-LFD (P = 0.004); however, there was no significant difference between RKO-HFD and WT-HFDmice (P = 0.3). These results, corroborating our previous findings on the measurement of mRNA transcripts for UCP1 inthe BAT, suggest that RAGE may contribute to altered energy expenditure and provide a protective effect against HFD byAger deletion (Ager -/-).

Preparation and Characterization of Long Circulating Liposomes Containing Total Saponins of Paris Polyphylla Smith / 中国药师

Objective:To prepare and characterize the PEGylated liposomes containing total saponins of Paris Polyphylla. Meth-ods:Using the size, PDI, zeta potential and encapsulation efficiency of the liposomes as the indicators, the influencing factors in the preparation were optimized. The particle size, PDI and zeta potential were studied by a Malvern Zetasizer, the morphology was ob-served under a TEM, and the stability was studied as well. Results:The particle size, PDI, zeta potential and encapsulation efficiency of the PEGylated liposomes was (109. 4 ± 32. 7) nm, (0. 171 ± 0. 036), ( -36. 7 ± 4. 5) mV and (93. 5 ± 3. 2) %, respectively. The liposomes were small spheres with smooth surface under the TEM. The long term stability studies showed that the liposomes were stable in 3 months after stored at 4℃. Conclusion:The preparation technology of the PEGylated liposomes containing total saponins of Paris Polyphylla is feasible, which can obtain liposomal preparations with high entrapment efficiency and good stability.