Current Issue : April - June Volume : 2021 Issue Number : 2 Articles : 6 Articles
Identification of molecules able to promote neuroprotective mechanisms can represent a promising therapeutic approach to neurodegenerative disorders including Huntington’s disease. Curcumin is an antioxidant and neuroprotective agent, even though its efficacy is limited by its poor absorption, rapid metabolism, systemic elimination, and limited blood–brain barrier (BBB) permeability. Herein, we report on novel biodegradable curcumin-containing nanoparticles to favor the compound delivery and potentially enhance its brain bioavailability. The prepared hyaluronan-based materials able to self-assemble in stable spherical nanoparticles, consist of natural fatty acids chemically conjugated to the natural polysaccharide. The aim of this study is to provide a possible effective delivery system for curcumin with the expectation that, after having released the drug at the specific site, the biopolymer can degrade to nontoxic fragments before renal excretion, since all the starting materials are provided by natural resource. Our findings demonstrate that curcumin-encapsulated nanoparticles enter the cells and reduce their susceptibility to apoptosis in an in vitro model of Huntington’s disease....
Several studies confirmed a correlation between elevated hydrogen peroxide (H2O2) levels in patients with intestinal bowel diseases (IBD) and the negative effects caused by its presence. The objective of this study was to explore the potential use of catalase (CAT) to diminish the level of H2O2 and its deleterious action on intestinal mucosa. Oral dosage forms of a CAT bioactive agent targeted to the intestines were designed and tested in various simulated gastric and intestinal media. Monolithic tablets (30% loading) were prepared using commercial CarboxyMethylCellulose (CMC) or synthesized CarboxyMethylStarch (CMS) and TriMethylAmineCarboxyMethylStarch (TMACMS) as matrix-forming excipients. For starch derivatives, the presence of the ionic groups (carboxymethyl and trimethylamine) was validated by spectral analysis. In vitro studies have shown that tablets formulated with TMACMS and 30% CAT resisted the acidity of the simulated gastric fluid and gradually released the enzyme into the simulated intestinal fluid. The investigation of the CAT release mechanism revealed the role of anionic and cationic groups of polymeric excipients and their involvement in the modulation of the CAT dissolution profile. The proposed drug delivery system can be considered an efficient solution to target CAT release in the intestine and contribute to the reduction of H2O2 associated with intestinal inflammation....
The aim of this work was to develop a mucoadhesive nanogel formulation containing nevirapine nanoparticles (NVP-Np) for potential use as a topical vaginal antiretroviral agent for prevention of HIV sexual transmission. NVP loaded nanoparticles were prepared by salting out method followed by incorporation in HPMC K100M gel bases to produce NVP-Np mucoadhesive nanogel. NVP-Np-loaded mucoadhesive nanogel included physicochemical characteristics, histopathology study, in-vitro cytotoxicity, gamma scintigraphy and in-vitro-in-vivo evaluations. Results of the histopathology study suggested that mucoadhesive nanogel containing NVP is safe therapy and improve the quality of life and reduce the side effect associated with vaginal infection. Results of the Scanning electron microscopy (SEM) studies revealed that the stability of the formulation which is in agreement with results found in Transmission electron microscopy (TEM) study. No cytotoxicity of the nanogel was detected in Hella cell lines. The in-vivo gamma scintigraphic study revealed that the optimized nanoparticles and mucoadhesive nanogel of NVP remained intact in the vagina for 12 h and 24 h respectively. The in-vivo pharmacokinetic studies revealed that the Cmax value of optimized nanoparticle and mucoadhesive nanogel of NVP was greater than the 0.5% CMC nanosuspension. NVP-Np based mucoadhesive nanogel was developed and characterized by physicochemical and biological characterization for providing protective drug levels at cervico vaginal tissues and HIV target cells for longer periods....
The purpose of this study was to prepare lipospheres drug delivery system for anti diabetic drug repaglinide with the aim of exploiting the favorable properties of this carrier system and developing a sustained release formula to defeat the side effects. Lipospheres using different ratio of bees wax, stearic acid, cetyl alcohol, tween 80 and phospholipids coat such as soybean phosphotidylcholine in various concentration was prepared in order to obtain new formulation containing repaglinide to reduce blood glucose level. Seven different formulations of lipospheres were prepared by melt dispersion technique. Lipospheres thus prepared were characterized for particle size, scanning electron microscopy, % entrapment efficiency, % yield, % drug content, in-vitro drug release and stability study. All the formulation gave the satisfactory result in terms of particle size, entrapment efficiency and drug content. Lipospheres were substantially stable after 3 months storage at 2–8°C. Repaglinide release from the lipospheres was depended on the ratio and type of the polymer used in the formulation. The best lipospheres performance and in-vitro drug release profile were achieved by using repaglinide, stearic acid and bees wax i.e. F4 formulation, this formulation shows drug release of 80.6±1.50 % at the end of 12 h....
This work is focused on the potential use of pulmonary surfactant to deliver full-length recombinant human surfactant protein SP-D (rhSP-D) using the respiratory air-liquid interface as a shuttle. Surfactant protein D (SP-D) is a collectin protein present in the pulmonary surfactant (PS) system, involved in innate immune defense and surfactant homeostasis. It has been recently suggested as a potential therapeutic to alleviate inflammatory responses and lung diseases in preterm infants suffering from respiratory distress syndrome (RDS) or bronchopulmonary dysplasia (BPD). However, none of the current clinical surfactants used for surfactant replacement therapy (SRT) to treat RDS contain SP-D. The interaction of SP-D with surfactant components, the potential of PS as a respiratory drug delivery system and the possibility to produce recombinant versions of human SP-D, brings the possibility of delivering clinical surfactants supplemented with SP-D. Here, we used an in vitro setup that somehow emulates the respiratory air-liquid interface to explore this novel approach. It consists in two different compartments connected with a hydrated paper bridge forming a continuous interface. We firstly analyzed the adsorption and spreading of rhSP-D alone from one compartment to another over the air-liquid interface, observing low interfacial activity. Then, we studied the interfacial spreading of the protein co-administered with PS, both at different time periods or as a mixed formulation, and which oligomeric forms of rhSP-D better traveled associated with PS. The results presented here demonstrated that PS may transport rhSP-D long distances over air-liquid interfaces, either as a mixed formulation or separately in a close window time, opening the doors to empower the current clinical surfactants and SRT....
Progressive increase in bacterial resistance has caused an urgent need to introduce new antibiotics, one of them being oxazolidinones with their representative tedizolid. Despite the broad spectrum of activity of the parent tedizolid, it is characterized by low water solubility, which limits its use. The combination of the active molecule with a multifunctional excipient, which is cyclodextrins, allows preservation of its pharmacological activity and modification of its physicochemical properties. Therefore, the aim of the study was to change the dissolution rate and permeability through the model membrane of tedizolid by formation of solid dispersions with a cyclodextrin. The research included identification of tedizolid-hydroxypropyl-β-cyclodextrin (tedizolid/HP-β-CD) inclusion complex by thermal method (Differential Scanning Colorimetry), spectroscopic methods (powder X-ray diffraction, Fourier-Transform Infrared spectroscopy), and molecular docking. The second part of the research concerned the physicochemical properties (dissolution and permeability) and the biological properties of the system in terms of its microbiological activity. An increase in the dissolution rate was observed in the presence of cyclodextrin, while maintaining a high permeation coefficient and high microbiological activity. The proposed approach is an opportunity to develop drug delivery systems used in the treatment of resistant bacterial infections, in which, in addition to modifying the physicochemical properties caused by cyclodextrin, we observe a favorable change in the pharmacological potential of the bioactives....
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