Formulation and Characterization of Ziprasidone Floating Pellets

The objective of this study is to design and evaluate Ziprasidone Floating pellets, which prolongs the release rate of the drug while extending the residence time of the drug within the body environment and without causing undeliterious effects to the subject. Ziprasidone and controlled matrix polymer granules were prepared by different granulation techniques in the ratio of 1:1, 1:1.5 and 1:2.Ziprasidone multi unit formulations comprising cellulose polymers were prepared by wet granulation technique, where as the Ziprasidone multi unit formulations comprising lipoidal / fatty polymers were prepared by melt granulation technique. Ziprasidone multi unit formulations with drug and polymer proportion as 1:1, F1 and F2 formulations consisting Cellulose polymers HPMC K4M and HPMC K100 respectively were prepared by wet granulation technique. Keywords: Ziprasidone, wet granulation, Floating pellets, melt granulation and polymer.

Production of Urea/Acetylated-ligninsulfonate Matrix as SRFs and Investigation the Effect of Hydrodynamic Conditions on the Release Rate Using Biot Number

Background: This study aimed to investigate the effect of the hydrodynamic condition on the release rate of urea/acetylated lignin sulfonate (Ac-LS) matrix as slow-release fertilizers (SRFs). Therefore, two models were developed using the mass transfer balance for the finite/infinite volume of fluids, solving finite integral transform/separation of a variable. In these models, the Biot number that verified the hydrodynamic condition appeared. Methods: In the experimental section, the urea/Ac-LS matrix fertilizer was produced. The morphological, thermal, chemical, and mechanical properties of the LS, Ac-LS, urea, and urea/Ac-LS matrix were analyzed using Fe-SEM, TGA, XRD, and SANTAM. Finally, the nitrogen release of the matrix fertilizer was investigated at 25°C for different impeller speeds. Results: The results showed that the thermal and mechanical resistance of urea/Ac-LS, with strong interaction, increased rather than pure urea or Ac-LS. The models were also validated using experimental data. The results further showed that in both states, the external resistance of the mass transfer decreased with increasing impeller speed, and the nitrogen release rate increased with increasing Biot number. Conclusion: It was also observed that, in a given hydrodynamic condition, initially, the release rate in the finite environment was less than the infinite; however, after a while, the type of environment did not affect the release rate

Coaxial electrospinning preparation and antibacterial property of polylactic acid/tea polyphenol nanofiber membrane

The polylactic acid (PLA)/tea polyphenol (TP) nanofiber membranes were prepared by coaxial electrospinning. The physical properties, antibacterial agent release, degradation, and antibacterial properties were investigated. Results demonstrated that stepwise and controlled antibacterial agent release profiles were achieved based on the core-shell configuration and disparate degradation rate of PLA and TP. The mechanical performance decreased with the increase of the TP content in the shell layer. The cumulative antibacterial agent release rate of nanofiber membranes with different TP content was different, while the antibacterial agent release trend was the same. The antibacterial agent release rate of the sample was the fastest at the initial stage from 2 h to 8 h, and then gradually slowed down after 24 h. In addition, the antibacterial activity of the PLA/TP nanofiber membranes was confirmed by the inhibition zone method against both Gram-positive ( Staphylococcus aureus) and Gram-negative ( Escherichia coli). Results showed that the antibacterial performance of PLA/TP nanofiber was intensified with the increasing content of TP, especially had better antibacterial performance against S. aureus.

pH-Responsive Liposomes of Dioleoyl Phosphatidylethanolamine and Cholesteryl Hemisuccinate for the Enhanced Anticancer Efficacy of Cisplatin

The current study aimed to develop pH-responsive cisplatin-loaded liposomes (CDDP@PLs) via the thin film hydration method. Formulations with varied ratios of dioleoyl phosphatidylethanolamine (DOPE) to cholesteryl hemisuccinate (CHEMS) were investigated to obtain the optimal particle size, zeta potential, entrapment efficiency, in vitro release profile, and stability. The particle size of the CDDP@PLs was in the range of 153.2 ± 3.08–206.4 ± 2.26 nm, zeta potential was −17.8 ± 1.26 to −24.6 ± 1.72, and PDI displayed an acceptable size distribution. Transmission electron microscopy revealed a spherical shape with ~200 nm size. Fourier transform infrared spectroscopic analysis showed the physicochemical stability of CDDP@PLs, and differential scanning calorimetry analysis showed the loss of the crystalline nature of cisplatin in liposomes. In vitro release study of CDDP@PLs at pH 7.4 depicted the lower release rate of cisplatin (less than 40%), and at a pH of 6.5, an almost 65% release rate was achieved compared to the release rate at pH 5.5 (more than 80%) showing the tumor-specific drug release. The cytotoxicity study showed the improved cytotoxicity of CDDP@PLs compared to cisplatin solution in MDA-MB-231 and SK-OV-3 cell lines, and fluorescence microscopy also showed enhanced cellular internalization. The acute toxicity study showed the safety and biocompatibility of the developed carrier system for the potential delivery of chemotherapeutic agents. These studies suggest that CDDP@PLs could be utilized as an efficient delivery system for the enhancement of therapeutic efficacy and to minimize the side effects of chemotherapy by releasing cisplatin at the tumor site.

Dendriplex-Impregnated Hydrogels With Programmed Release Rate

Hydrogels are biocompatible matrices for local delivery of nucleic acids; however, functional dopants are required to provide efficient delivery into cells. In particular, dendrimers, known as robust nucleic acid carriers, can be used as dopants. Herein, we report the first example of impregnating neutral hydrogels with siRNA–dendrimer complexes. The surface chemistry of dendrimers allows adjusting the release rate of siRNA-containing complexes. This methodology can bring new materials for biomedical applications.