ABSTRACT
In this study, mesoporous SnO2 (MSn) with a three-dimensional mesoporous structure was prepared using MCM-48 as the template in order to increase the oral bioavailability and dissolution rate of insoluble drugs. The model drug, nitrendipine (NDP), was loaded into the MSn by the adsorption method. The structural features of MSn were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), and N2 adsorption (desorption) analysis. NDP was existed in the pore channels of MSn in an amorphous state, which was characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). MSn showed a good biocompatibility in the cell toxicity assay for Caco-2 cells. In vitro dissolution results suggested that MSn could significantly enhance the dissolution rate of NDP compared with commercial NDP tablets. Pharmacokinetic studies indicated that NDP-MSn tablets effectively enhanced the oral bioavailability of NDP. In conclusion, MSn was found to be a potential carrier for improving the solubility of insoluble drugs.
Subject(s)
Nitrendipine/chemistry , Tin Compounds/chemistry , Administration, Oral , Animals , Biological Availability , Caco-2 Cells , Drug Carriers , Humans , Nitrendipine/pharmacokinetics , Porosity , Rabbits , SolubilityABSTRACT
BACKGROUND: Biopharmaceutics classification system class II drugs have low solubility, which limits their extent and speed of absorption after oral administration. Over the years, mesoporous materials have been widely used to increase the dissolution rate and oral relative bioavailability of poorly water-soluble drugs. OBJECTIVES: In order to improve the dissolution rate and increase oral relative bioavailability of the poorly water-soluble drugs, a tin oxide carrier (MSn) with a mesoporous structure was successfully synthesized. METHODS: In this study, MSn was synthesized using mesoporous silica material (SBA-15) as the template. Fenofibrate (FNB) was adsorbed into the channels of MSn by an adsorption method. Characterizations of the pure FNB, MSn, physical mixture of the drug and MSn (PM; 1:1) and FNB-loaded MSn (FNB-MSn) samples were carried out by the scanning electron microscopy (SEM), transmission electron microscopy (TEM), N2 adsorption/desorption, powder X-ray diffractometer (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopy. Cytotoxicity assay (MTT) was used to evaluate the cytotoxicity of MSn. In vitro dissolution studies were performed to investigate the dissolution rate of FNB-MSn. In vivo pharmacokinetic studies were used to investigate the changes of plasma drug concentrations of FNB-MSn tablets and commercial FNB tablets in rabbits. RESULTS: Detailed characterization showed that FNB in the channels of MSn was present in an amorphous state. The in vitro release tests demonstrated that MSn with a good biocompatibility could effectively enhance the dissolution rate of FNB. Pharmacokinetic results indicated that MSn significantly increased the oral relative bioavailability of FNB. CONCLUSION: MSn can be regarded as a promising carrier for an oral drug delivery system.
Subject(s)
Fenofibrate/chemistry , Fenofibrate/pharmacokinetics , Tin Compounds/chemistry , Administration, Oral , Animals , Biological Availability , Caco-2 Cells , Drug Carriers/chemical synthesis , Drug Carriers/chemistry , Fenofibrate/administration & dosage , Humans , Particle Size , Porosity , Rabbits , Solubility , Surface Properties , Tin Compounds/chemical synthesisABSTRACT
In this study, we prepared PTX-loaded mesoporous hollow SnO2 nanofibers conjugated with folic acid (SFNFP) for liver cancer therapy. According to SEM and TEM characterization, SFNF showed a mesoporous hollow structure. The average outer diameter was 200 nm, and the wall thickness was 50 nm. The DSC and XRD study showed that PTX in the channels of nanofibers was present in an amorphous state. The in vitro release experiments demonstrated that SFNF could efficiently improve the dissolution rate of PTX. Both in vitro cell experiments and in vivo antitumor experiments showed that SFNFP could efficiently inhibit the growth of liver cancer cells. Therefore, SFNF is a promising targeting antitumor drug delivery carrier.
Subject(s)
Antineoplastic Agents/chemistry , Drug Carriers/chemistry , Folic Acid/chemistry , Nanofibers/chemistry , Paclitaxel/chemistry , Tin Compounds/chemistry , Animals , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Drug Delivery Systems/methods , Female , Humans , Liver Neoplasms/drug therapy , Mice , Nanoparticles/chemistry , Paclitaxel/pharmacologyABSTRACT
In this study, biodegradable chitosan hollow nanospheres (CHN) were fabricated using polystyrene nanospheres (PS) as templates. CHN were applied to increase the solubility of poorly water-soluble drugs. The lung cancer drug paclitaxel (PTX), which is used as a model drug, was loaded into CHN by the adsorption equilibrium method. The drug-loaded sample (PTX-CHN) offered sustained PTX release and good bioavailability. The state characterization of PTX by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) showed that the PTX absorbed into CHN existed in an amorphous state. An in vitro toxicity experiment indicated that CHN were nontoxic as carriers of poorly water-soluble drugs. The PTX-CHN produced a marked inhibition of lung cancer A549 cells proliferation and encouraged apoptosis. A cell uptake experiment indicated that PTX-CHN was successfully taken up by lung cancer A549 cells. Furthermore, a degradation experiment revealed that CHN were readily biodegradable. These findings state clearly that CHN can be regarded as promising biomaterials for lung cancer treatment.
