Photoprotective, biological activities and chemical composition of the non-toxic hydroalcoholic extract of Clarisia racemosa with cosmetic and pharmaceutical applications

作者: de Lima, Maria do Carmo Alves ; silva, Pollyne amorim ; Pereira, Daniel Tarciso Martins ; Rocha, Wilma Raianny Vieira da ; da Silva, Abdenego Rodrigues ; da Silva Abreu, Alcicley ; Albuquerque Nerys, Lais Ludmila de ; da Cruz Filho, Iranildo Jose ; Jacob, Iris Trindade Tenorio ; da Silva, Rosali Maria Ferreira ; de Oliveira, Alisson Macario

Clarisia racemosa (guariuba), Moraceae, is a native tree of the Amazon region, with timber value in the local market and for export.Aiming to contribute to the biol. study of the crude extract, we carried out its hydroalcoholic extraction and physicochem. characterization.The results showed that the wood had the following chem. composition: cellulose (40.1%), hemicellulose (18.34%), lignin (29.40%), extractives (10.7%), and ash (0.79%).The extract obtained showed a high content of phenolics and through liquid chromatog. tests, it was possible to determine 17 compoundsTherefore, we evaluated its biol. properties (antioxidant, antiglycant, in vitro and in vivo toxicity, antitumor, antimicrobial and photoprotective) to use it as a raw material in cosmetic and pharmaceutical formulations.The extract showed moderate antioxidant activity, it was also able to inhibit antiglycant reactions.And it showed no toxic effects in vitro and in vivo assays.Highlighting antiproliferative activity against MCF-7, T47D, DU-145, and Jurkat tumor cells.As reported in the literature, these models are still being used as a predictor of cytotoxicity.Regarding the in vitro antimicrobial assays, the extract showed activity against Staphylococcus aureus with a minimal inhibitory concentration similar to the oxacillin pattern.Finally, it was able to promote photoprotective activity in vitro at non-toxic concentrationsThis study shows the potential of the hydroalcoholic extract of Clarisia racemosa to be used as a component in cosmetic and pharmaceutical formulations.

2020-04-01·Journal of Controlled Release1区 · 医学

Size-adaptable and ligand (biotin)-sheddable nanocarriers equipped with avidin scavenging technology for deep tumor penetration and reduced toxicity

1区 · 医学

Article

作者: Jin, Ya ; Chu, Xinyu ; Zi, Yixuan ; Wu, Zimei ; Liu, Jianping ; Wu, Chenchen ; Zhang, Wenli

The conventional active-targeting nano-chemotherapy suffers from poor tumor tissue penetration and non-negligible toxicity due to the size/ligand dilemmas and insufficient target selectivity. In this report, a stimuli-responsive size-adaptable and ligand (biotin)-sheddable drug delivery system (DDS) combined with two-step strategy of biotin-avidin system was designed to seek a balance between tumor targeting and penetration as well as to self-scavenge the nonresponsive nanocarriers in normal tissues. This DDS was composed of 'multi-seed' polymeric liposomes (ASL-BIO-MPL) with asulacrine-loaded micelles as seeds in their aqueous cavities. The shell of such liposomes was modified with MMP-9 cleavable polymer-polypeptide functionalized with the tumor targeting ligand biotin. ASL-BIO-MPL could disintegrate into mixture of irregularly-shaped liposomes (~200 nm) and scattered tiny micelles (~40 nm) after incubation with MMP-9. The fluorescence-labeled BIO-MPL could travel to the center of the 4T1 breast tumor spheroids under the action of MMP-9, possibly benefited from the relay of released tiny micelles. Conversely, neither the biotin-modified micelles nor non-MMP-9-responsive multi-seed liposomes could penetrate into the spheroids possibly due to the potent binding-site barrier of biotin and large size, respectively. In tumor-bearing mice, ASL-BIO-MPL exhibited the strongest drug penetrability and thus the optimal inhibition of tumor growth compared to other formulations. Following administration of avidin with a rational dosage regimen, the number of apoptotic cells in normal tissues induced by ASL-BIO-MPL reduced without affecting their targeting effect, suggesting the followed administration of adivin could scavenge the DDS in non-target site. Overall, the size/ligand adapting MPL system combined with two-step strategy of biotin-avidin may provide potential avenues for nanocarriers to enhance deep tumor tissue targeting and protect normal tissues.

2018-01-01·Drug Delivery2区 · 医学

Multiseed liposomal drug delivery system using micelle gradient as driving force to improve amphiphilic drug retention and its anti-tumor efficacy

2区 · 医学

ArticleOA

作者: Jin, Ya ; Wu, Zimei ; Baguley, Bruce C. ; Liu, Jianping ; Li, Caibin ; Shaw, John P. ; Wang, Zhiyu ; Liu, Xinyue ; Zhang, Wenli

To improve drug retention in carriers for amphiphilic asulacrine (ASL), a novel active loading method using micelle gradient was developed to fabricate the ASL-loaded multiseed liposomes (ASL-ML). The empty ML were prepared by hydrating a thin film with empty micelles. Then the micelles in liposomal compartment acting as 'micelle pool' drove the drug to be loaded after the outer micelles were removed. Some reasoning studies including critical micelle concentration (CMC) determination, influencing factors tests on entrapment efficiency (EE), structure visualization, and drug release were carried out to explore the mechanism of active loading, ASL location, and the structure of ASL-ML. Comparisons were made between pre-loading and active loading method. Finally, the extended drug retention capacity of ML was evaluated through pharmacokinetic, drug tissue irritancy, and in vivo anti-tumor activity studies. Comprehensive results from fluorescent and transmission electron microscope (TEM) observation, encapsulation efficiency (EE) comparison, and release studies demonstrated the formation of ML-shell structure for ASL-ML without inter-carrier fusion. The location of drug mainly in inner micelles as well as the superiority of post-loading to the pre-loading method , in which drug in micelles shifted onto the bilayer membrane was an additional positive of this delivery system. It was observed that the drug amphiphilicity and interaction of micelles with drug were the two prerequisites for this active loading method. The extended retention capacity of ML has been verified through the prolonged half-life, reduced paw-lick responses in rats, and enhanced tumor inhibition in model mice. In conclusion, ASL-ML prepared by active loading method can effectively load drug into micelles with expected structure and improve drug retention.

100 项与 Asulacrine Isethionate 相关的药物交易

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