Synthesis and In Vitro Characterization of Carboxymethyl Chitosan-CBA-Doxorubicin Conjugate Nanoparticles as pH-Sensitive Drug Delivery Systems

2017 ◽  
Vol 13 (9) ◽  
pp. 1097-1105 ◽  
Author(s):  
Rui Hu ◽  
Hua Zheng ◽  
Jun Cao ◽  
Zahra Davoudi ◽  
Qun Wang
Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1052
Author(s):  
Reem Abou Assi ◽  
Ibrahim M. Abdulbaqi ◽  
Toh Seok Ming ◽  
Chan Siok Yee ◽  
Habibah A. Wahab ◽  
...  

Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.


2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Pankajkumar S. Yadav ◽  
Ekta Yadav ◽  
Amita Verma ◽  
Saima Amin

The objective of the current work was to develop optimized self-nanoemulsifying drug delivery systems (SNEDDS) and evaluate theirin vitroandin vivoperformance. The research comprised various studies which includes solubility studies in various vehicles, pseudoternary phase diagram construction, and preparation and characterization of SNEDDS along within vitrodissolution andin vivopharmacodynamic profiling. Based on dissolution profile, a remarkable increase in rate of dissolution was observed in comparison with plain drug and marketed formulation. Optimized SNEDDS formulation was composed of Capmul MCM (19.17% w/w), Tween 80 (57.5% w/w), Transcutol P (12.7% w/w), and HCT (4.17% w/w).In vivopharmacodynamic evaluation in Wistar rats showed considerable increase in pharmacological effect of HCT by SNEDDS formulation as compared with plain HCT.


2018 ◽  
Vol 32 (8) ◽  
pp. 1105-1118 ◽  
Author(s):  
Qingqing Sang ◽  
Heyu Li ◽  
Gareth Williams ◽  
Huanling Wu ◽  
Li-Min Zhu

Dual-drug-loaded pH-responsive fiber scaffolds were successfully prepared by coaxial electrospinning. These were designed with the aim of being sutured into the resection site after tumor removal, to aid recovery and prevent cancer recurrence. The shell was made up of a mixture of gelatin and sodium bicarbonate (added to provide pH-sensitivity), and was loaded with the anti-inflammatory drug ciprofloxacin; the core comprised poly(lactide-co-ε-caprolactone) with the chemotherapeutic doxorubicin hydrochloride. Scanning electron microscopy revealed most fibers were smooth and homogeneous. Transmission electron microscopy demonstrated the presence of a clear core/shell structure. The fiber scaffolds were further characterized using infrared spectroscopy and X-ray diffraction, which proved that both drugs were present in the fibers in the amorphous form. The gelatin shells were cross-linked with glutaraldehyde to enhance their stability, and water contact angle measurements used to confirm they remained hydrophilic after this process, with angles between 10 and 35°. This is important for onward applications, since a hydrophilic surface is known to encourage cell proliferation. During in vitro drug release studies, a rapid and acid-responsive release of ciprofloxacin was seen, accompanied by sustained and long-term doxorubicin release. Both the release profiles and the mechanical strength of the fibers can effectively be tuned through the sodium bicarbonate content of the fibers: for instance, the break stress varies from 2.00 MPa to 2.57 MPa with an increase in sodium bicarbonate content. The pH values of aqueous media exposed to the scaffolds decrease only slightly, by less than 0.5 pH units, over the two-month timescale, suggesting that only minimal fiber degradation occurs during this time. The fiber scaffolds also have good biocompatibility, as revealed by in vitro cytotoxicity experiments. Overall, our results demonstrate that the novel scaffolds reported here are promising pH-sensitive drug delivery systems, and may be candidates for use after tumor resection surgery.


2015 ◽  
Vol 11 (6) ◽  
pp. 964-978 ◽  
Author(s):  
Wenchuan She ◽  
Dayi Pan ◽  
Kui Luo ◽  
Bin He ◽  
Gang Cheng ◽  
...  

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