scholarly journals A Solid Ultra Fine Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) of Deferasirox for Improved Solubility: Optimization, Characterization, and In Vitro Cytotoxicity Studies

2020 ◽  
Vol 13 (8) ◽  
pp. 162 ◽  
Author(s):  
Alaa Alghananim ◽  
Yıldız Özalp ◽  
Burcu Mesut ◽  
Nedime Serakinci ◽  
Yıldız Özsoy ◽  
...  

The research work was designed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox (DFX). According to the solubility studies of DFX in different components, Peceol, Kolliphor EL, and Transcutol were selected as excipients. Pseudo-ternary phase diagrams were constructed, and then SNEDDS formation assessment studies and solubility of DFX in selected SNEDDSs formulations were performed. DFX loaded SNEDDS were prepared and characterized. The optimum DFX-SNEDDS formulations were developed. The relative safety of the optimized SNEDDS formulation was examined in a human immortalized myelogenous leukemia cell line, K562 cells, using the MTT cell viability test. Cytotoxicity studies revealed more cell viability (71.44%) of DFX loaded SNEDDS compared to pure DFX (3.99%) at 40 μM. The selected DFX-SNEDDS formulation was converted into S-SNEDDS by adsorbing into porous carriers, in order to study its dissolution behavior. The in vitro drug release studies indicated that DFX release (Q5%) from S-SNEDDS solidified with Neusilin UFL2 was significantly higher (93.6 ± 0.7% within 5 min) compared with the marketed product (81.65 ± 2.10%). The overall results indicated that the S-SNEDDS formulation of DFX could have the potential to enhance the solubility of DFX, which would in turn have the potential to improve its oral bioavailability as a safe novel delivery system.

Dose-Response ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 155932582092673
Author(s):  
Chuan Xie ◽  
Yan Zhan ◽  
Peng Wang ◽  
Bo Zhang ◽  
Yukun Zhang

Adipic dihydrazide and heparin were attached to ZnO quantum dots surface, and the ZnO-adipic dihydrazide-heparin nanocomplex was used as a drug delivery system to deliver paclitaxel for chemotherapy. The surface modification and the loading of paclitaxel were confirmed by Fourier transform infrared spectrum, featured by characteristic peaks from functional groups of adipic dihydrazide, heparin, and paclitaxel. The impacts of pH on the drug release were investigated, and the cytotoxicity studies were conducted with A549 cells. The pharmacokinetic study was conducted with male Wistar rats. Both in vitro and in vivo study indicated that ZnO-adipic dihydrazide-heparin-paclitaxel nanocomplex could deliver paclitaxel in a more controllable way, and it has the potential to be a high-efficiency drug delivery system for cancer treatment.


2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Leslie Raphael de Moura Ferraz ◽  
Alinne Élida Gonçalves Alves Tabosa ◽  
Débora Dolores Souza da Silva Nascimento ◽  
Aline Silva Ferreira ◽  
Victor de Albuquerque Wanderley Sales ◽  
...  

Abstract Chagas disease (CD), caused by the flagellate protozoan Trypanosoma cruzi, is one of the major public health problems in developing countries. Benznidazole (BNZ) is the only drug available for CD treatment in most countries, however, it presents high toxicity and low bioavailability. To address these problems this study used Zeolitic Imidazolate Framework-8 (ZIF-8), which has garnered considerable attention due to its potential applications, enabling the controlled delivery of drugs. The present work developed and characterized a BNZ@ZIF-8 system, and the modulation of BNZ release from the ZIF-8 framework was evaluated through the in vitro dialysis release method under sink conditions at different pH values. Moreover, the in vitro evaluation of cell viability and cytotoxicity by MTT assay were also performed. The dissolution studies corroborated that a pH sensitive Drug Delivery System capable of vectorizing the release of BNZ was developed, may leading to the improvement in the bioavailability of BNZ. The MTT assay showed that no statistically significant toxic effects occurred in the developed system, nor significant effects on cell viability.


2020 ◽  
Vol 10 (3-s) ◽  
pp. 43-46
Author(s):  
Dipali Trivedi ◽  
Arti Majumdar ◽  
Neelesh Malviya

Besides enormous improvements in drug delivery, oral route has been highly and effectively utilized route of administration. Floating drug delivery that is also known to be low density system is advancement in the class of gastro-retentive drug delivery system. In the present research work, floating drug delivery of Rilpivirine hydrochloride was developed by overcoming various limitations and troubles associated with the drug including poor absorption in intestinal pH and degradation when comes in contact with higher pH environment. [2] Prepared formulations were evaluated for various parameters like friability, hardness, thickness, drug content analysis, floating properties and in-vitro drug release study. Based on the evaluation, concluded that floating drug delivery system is a non-toxic as well as cost-effective technique for the rationale of enhancing bioavailability and absorption of poorly water soluble drugs. The improvement in gastric residence time is a clear sign. It can be able to use in the future for more acidic soluble drugs to enhance solubility and absorption. Keywords: Floating drug delivery, gastric residence time, Rilpivirine, effervescent, NNRTI.


2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 


Sign in / Sign up

Export Citation Format

Share Document