Development of thalidomide-loaded biodegradable devices and evaluation of the effect on inhibition of inflammation and angiogenesis after subcutaneous application (original) (raw)
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European Journal of Pharmaceutics and Biopharmaceutics, 2009
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International journal of nanomedicine, 2018
Thalidomide (THA) is an angiogenesis inhibitor and an efficient inhibitor of the tumor necrosis factor-α (TNF-α). However, the clinical application of THA has been limited due to hydrophobicity of the compound. To increase the water solubility of THA and in order to evaluate the anticancer abilities of this material on human lung carcinoma, methoxy poly(ethylene glycol)-poly(ε-caprolactone) nanoparticles loaded with THA (THA-NPs) were prepared. The synthesis of THA-NPs was carried out via a dialysis method with relative satisfactory encapsulation efficiency, loading capacity, size distribution, and zeta potential. A cytotoxicity assay demonstrated that THA-NPs inhibited the growth of cells in a dose-dependent manner. The evaluation of anti-tumor activity in vivo showed that THA-NPs could inhibit tumor growth and prolong the survival rate of tumor-bearing mice. Immunohistochemical analysis indicated that THA-NPs inhibited cell proliferation (Ki-67 positive rate, 32.8%±4.2%, <0.01)...
Biomaterial implants in the treatment of oncology: a review
International Journal of Basic & Clinical Pharmacology, 2021
In globally, cancer is a second leading disease next to cardiovascular diseases in non-communicable diseases, which affect the all ages, sex, social status, ethnicity and primary cause of illness related death. Traditionally, systemic delivery drug systems like chemotherapy via oral capsule, injections of nanoparticles/micro particles, immunotherapy and others, which can inhibit or halt the progression of tumors. The short half-life of drugs which cannot achieve the targeted dose level to the tumor site and not able to target desired cell and commonly produces the organ toxicity. Recently, researchers have been attempting to direct delivery agents for cancer therapy. One of the best methods is a local therapy system, which deliver the drug directly via implantable procedure and it’s achieved the maximum concentration of the desire drug at the tumor site, non-target systemic exposure and minimize the organ toxicity to the patients. Biomaterial implants are widely used in the local co...
Percutaneous Delivery of Thalidomide and Its N-Alkyl Analogs
Pharmaceutical Research, 2002
Purpose. The purpose of this study was to determine the permeation parameters of thalidomide and three of its N-alkyl analogs and to establish a correlation between the physicochemical properties of these compounds and their percutaneous rates of absorption. Methods. In vitro permeation studies were performed from buffer, n-alkanols and various mixed components using vertical Franz diffusion cells fitted with human epidermal membranes. Results. Measured steady-state fluxes indicate that N-methyl thalidomide is a far better penetrant of human skin than the “parent molecule”. However, fluxes through skin drop off markedly from that of the methylated compound when the chain length is extended to propyl and pentyl. However, they remain well above the flux of thalidomide, which is less than 0.025 μg/cm2/h. Conclusions. The best skin permeant of this series was the N-methyl analog, which also exhibited the highest water (buffer) solubility compared to thalidomide, and the N-propyl and N-pentyl analogs. The N-propyl and N-pentyl analogs were more lipid soluble and exhibited higher partition coefficient values than the N-methyl analog. From all the permeability data using buffer, a series of n-alkanols and various combinations of solvents and enhancers as vehicles, the more water-soluble compound and not the more lipid soluble one was the best skin permeant.