Current Issue : April-June Volume : 2023 Issue Number : 2 Articles : 5 Articles
A key challenge in treating solid tumors is that the tumor microenvironment often inhibits the penetration of therapeutic antibodies into the tumor, leading to reduced therapeutic efficiency. It has been reported that the combination of ultrasound-responsive micro/nanobubble and therapeutic ultrasound (TUS) enhances the tissue permeability and increases the efficiency of delivery of macromolecular drugs to target tissues. In this study, to facilitate efficient therapeutic antibody delivery to tumors using this combination system, we developed therapeutic antibody-modified nanobubble (NBs) using an Fc-binding polypeptide that can quickly load antibodies to nanocarriers; since the polypeptide was derived from Protein G. TUS exposure to this Herceptin®-modified NBs (Her-NBs) was followed by evaluation of the antibody’s own ADCC activity, resulting the retained activity. Moreover, the utility of combining therapeutic antibody-modified NBs and TUS exposure as an antibody delivery system for cancer therapy was assessed in vivo. The Her-NBs + TUS group had a higher inhibitory effect than the Herceptin and Her-NBs groups. Overall, these results suggest that the combination of therapeutic antibody-modified NBs and TUS exposure can enable efficient antibody drug delivery to tumors, while retaining the original antibody activity. Hence, this system has the potential to maximize the therapeutic effects in antibody therapy for solid cancers....
To improve the powder properties of active pharmaceutical ingredients (APIs), we coated APIs with silica nanoparticles using a dry process that allowed for direct compression into tablets. The dry coating performed with different apparatuses (a batch-type high-speed shear mixer (Mechanomill) and a continuous conical screen mill (Comil)) and properties of the resulting dry-coated APIs were compared. Ethenzamide (ETZ), which has low powder flowability, was selected as the host particle to be improved and the colloidal silicas Aerosil 200 and R972 were used as the guest particles. Both coating processes and types of silica nanoparticles improved the powder flowability (angle of repose) of ETZ under unstressed conditions. Inverse gas chromatography demonstrated that dry coating with silica nanoparticles reduced the surface free energy and improved the homogeneity of the surface energy distribution of ETZ particles. Under the stress conditions of a shear cell test, the Mechnomillbased treatment improved the powder flowability of ETZ from that of untreated ETZ; however, the Comil-based treatment did not improve the flowability. The mechanical shear force exerted by Comil was apparently insufficient for interactions between host and guest particles. However, the properties of tableted ETZ were enhanced even when the silica nanoparticles were coated using Comil....
Process Analytical Technology (PAT) has been increasingly used in the pharmaceutical industry to monitor essential parameters in real-time during pharmaceutical processes. The concentration of Active Pharmaceutical Ingredients (APIs), such as paracetamol, is one of these parameters, and controlling its variations allows for optimization of the production process. In this study, a refractometric sensor, implemented by an interrogation system based on an Erbium-Doped Fiber Ring Cavity (EDFRC), was presented and experimentally demonstrated. The Cavity Ring proposed included a 1 × 3 coupler. One port of the coupler was used to increase the optical power of the system through a Fiber Bragg Grating (FBG), and the other two ports were used as sensing head and reference. The sensor detected variations of paracetamol concentration with a sensitivity of [(−1.00 ± 0.05) × 10−3] nW/(g/kg) and a resolution of 5.53 g/kg. The results demonstrate the potential of this technology as a possible non-invasive PAT tool....
In order to improve the stability of oxytetracycline hydrochloride, a polymorphic antibiotic set of novel binary systems were developed using β-cyclodextrin and amino acids with different acidbasic characteristics as ligands. The formation constants for each system containing β-cyclodextrin, Laspartic acid, histidine and N-acetylcysteine were determined by Scott’s method and statistical studies. The structure of the binary systems with β-cyclodextrin and N-acetylcysteine was elucidated by NMR experiments. The effect β-cyclodextrin and N-acetylcysteine on the polymorph’s chemical stability in aqueous and phosphate buffered saline solutions at 25 ◦C was monitored by an optimized and validated high-performance liquid chromatography method. The combination of N-acetylcysteine with the three polymorphs and the β-cyclodextrin system obtained with the form III demonstrated a reduction in the degradation rate of oxytetracycline hydrochloride in the aqueous solution when compared to each free form, with an increase of 20 h in the half time. It evidences that the use of amino acids as ligands constitutes an interesting alternative for pharmaceutical areas. In conclusion, based on the results obtained, these pharmaceutical systems could be candidates for the development of a pharmaceutical formulation for the administration of the drug through reconstituted solutions using the binary system as a promising tool for improving the stability of oxytetracycline hydrochloride polymorphs in solution....
Spray drying is a promising technology for drying lipid nanodispersions. These formulations can serve as carrier systems for poorly water-soluble active pharmaceutical ingredients (APIs) that are loaded into the lipid matrix to improve their bioavailability. Once the API-loaded nanocarriers have been further processed into solid dosage forms, they could be administered orally, which is usually preferred by patients. Various solid lipids as well as oils were used in this study to prepare lipid nanodispersions, and it was shown that their nanoparticulate properties could be maintained when lactose in combination with SDS was used as matrix material in the spray-drying process. In addition, for lipid nanoemulsions loaded with fenofibrate, a good redispersibility with particle sizes below 300 nm at a lipid content of 26.8 wt.% in the powders was observed. More detailed investigations on the influence of the drying temperature yielded good results when the inlet temperature of the drying air was set at 110 ◦C or above, enabling the lactose to form an amorphous matrix around the embedded lipid particles. A tristearin suspension was developed as a probe to measure the temperature exposure of the lipid particles during the drying process. The results with this approach indicate that the actual temperature the particles were exposed to during the drying process could be higher than the outlet temperature....
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