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Targeted Drug Delivery Systems (TDDS) have attracted wide attention with reduced drug side effects and improved anti-tumor efficacy in comparison with traditional preparations. While targeting moiety in existing TDDS principally focused on recognition of receptors on the surface of tumor cells, accumulation into tumor tissue only could be performed by enhanced permeability and retention effect and active transportation into tumor cells. Doxorubicin (DOX)-loaded sialic acid-dextran (Dex)-octadecanoic acid (OA) micelles (SA-Dex-OA/DOX) were designed for targeting hepatocellular carcinoma effectively. The synthesized conjugates could self-aggregate to form micelles with a critical micelle concentration of 27.6 μg·mL-1 and diameter of 54.53±3.23 nm. SA-Dex-OA micelles incorporated with 4.36% DOX loading content could prolong in vitro drug release to 96 h with 80 % of final release. Cellular transportation studies revealed that SA-Dex-OA micelles mediated more efficient DOX delivery into Bel-7402 cells than those without SA modification. In vivo biodistribution test demonstrated that SA-Dex-OA/ICG micelles showed 3.05-fold higher accumulation into Bel-7402 tumors. The recognition of overexpressed E-selectin in inflammatory tumor vascular endothelial cells led to large accumulation of SA-Dex-OA/ICG micelles into tumor tissue, and the E-selectin upregulated on the surface of tumor cells contributed to active cellular transportation into tumor cells. Accordingly, SA-Dex-OA/DOX exhibited prior suppression on Bel-7402 tumor growth to Dex-OA/DOX micelles and free DOX (the tumor inhibition: 79.2 % vs 61.0 % and 51.3%). These results suggest that SA-functionalized micelles with dual targeting properties has high potential for liver cancer therapy.
This article was published in the following journal.
Name: Molecular pharmaceutics
Tumor-targeting micelles for the delivery of paclitaxel (PTX) were developed based on folic acid and α-tocopherol succinate conjugated hyaluronic acid (FA-HA-TOS). The conjugate FA-HA-TOS was synthes...
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An efficient streamlined chemoenzymatic approach has been developed for gram-scale synthesis of Lewis a angtigen (LeβProN) and a library of sialyl Lewis a antigens (sLeβProN) containing different si...
This study is aimed at assessing the impact of short-term (3 days) exogenous sialic acid supplementation on endogenous biomarkers of sialic acid metabolism in NANS deficient patients.
Sialic acid (SA) is the generic term given to a family of acetylated derivatives of neuraminic acid. SA is a 9 carbon monosaccharide. An important function of host SA is to regulate innate...
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Particles consisting of aggregates of molecules held loosely together by secondary bonds. The surface of micelles are usually comprised of amphiphatic compounds that are oriented in a way that minimizes the energy of interaction between the micelle and its environment. Liquids that contain large numbers of suspended micelles are referred to as EMULSIONS.
A graphic device used in decision analysis, series of decision options are represented as branches (hierarchical).
Autosomal recessive neurodegenerative disorders caused by lysosomal membrane transport defects that result in accumulation of free sialic acid (N-ACETYLNEURAMINIC ACID) within the lysosomes. The two main clinical phenotypes, which are allelic variants of the SLC17A5 gene, are ISSD, a severe infantile form, or Salla disease, a slowly progressive adult form, named for the geographic area in Finland where the kindred first studied resided.
A family of SIALIC ACID binding proteins found in vertebrate species. They are transmembrane proteins which act as cell surface receptors for a variety of sialylated GLYCOCONJUGATES. While a subset of siglec protein subtypes are evolutionarily conserved between mammalian species, there are many others that are species specific.
A sialic acid binding lectin that was originally identified as an adhesion molecule for inflammatory MACROPHAGES and activated MONOCYTES. This protein is the largest known siglec subtype and contains 16 immunoglobulin C2-set domains. It plays a role in cell to cell interactions and interactions with BACTERIA.
<!--LGfEGNT2Lhm-->Drug delivery is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. <!--LGfEGNT2Lhm-->Drug delivery technologies are <!--LGfEGNT2Lhm-->patent pr...
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...