scholarly journals Improvement of the Bioavailability and Anti-Hepatic Alveolar Echinococcosis by Albendazole-Isethionate/Hypromellose Acetate Succinate (HPMC-AS) Complex

2021 ◽  
Author(s):  
Chunhui Hu ◽  
Fabin Zhang ◽  
Haining Fan
Keyword(s):  
Oral Bioavailability ◽  
Alveolar Echinococcosis ◽  
Ph Value ◽  
Commercial Product ◽  
Dissolution Behavior ◽  
Aqueous Environment ◽  
Intrinsic Dissolution ◽  
Hepatic Alveolar Echinococcosis ◽  
Long Term Treatment ◽  
Hypromellose Acetate Succinate

Maximizing the pharmacodynamics of albendazole (ABZ), which is used to treat echinococcoses, is essential for the long-term treatment of echinococcosis patients. ABZ is a weak base whose solubility depends on the pH value of the solvent. After it has been orally administered, its solubility drops sharply from when it is in gastric juices (pH 1.4) to intestinal juices (pH 6.5) and is subsequently absorbed in the ileum and jejunum. This results in low solubility and poor bioavailability of the drug. In this study, we developed an orally administered albendazole-isethionate (ABZ-HES)/Hypromellose Acetate Succinate (HPMC-AS) complex tablet with improved solubility and bioavailability. Previous studies demonstrated that ABZ-HES has a higher intrinsic dissolution rate under pH 1.4 than the ABZ freebase used in the commercial product Albenda® and that HPMC-AS can effectively inhibit ABZ crystallization, which could be due to the hydrophobic interaction between ABZ and HPMC-AS in an aqueous environment. In this study, the dissolution behavior of ABZ-HES/HPMC-AS composite tablets (TABZ-HES-H) in vitro was studied by the two-step pH conversion method. Our results demonstrated that the oral bioavailability of TABZ-HES-H is approximately 2.6 times higher than that of ABZ. More importantly, in the rat model of secondary hepatic alveolar echinococcosis, the anti-hepatic alveolar echinococcosis effect of the TABZ-HES-H is 3.4 times higher than that of a commercial product. The improved preparation with salt and polymer has proven to be a feasible method of improving oral bioavailability and pharmacodynamics of ABZ.

scholarly journals Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1210
Author(s):  
Xieguo Yan ◽  
Shiqiang Wang ◽  
Kaoxiang Sun
Keyword(s):  
Drug Loading ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
In Vivo Evaluation ◽  
Long Term Treatment ◽  
Long Acting

Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term risperidone (RIS) implantation system that can stabilize RIS release and established in-vitro and in-vivo evaluation systems. Cumulative release, drug loading, and entrapment efficiency were used as evaluation indicators to evaluate the effects of different pore formers, polymer ratios, porogen concentrations, and oil–water ratios on a RIS implant (RIS-IM). We also built a mathematical model to identify the optimized formulation by stepwise regression. We also assessed the crystalline changes, residual solvents, solubility and stability after sterilization, in-vivo polymer degradation, pharmacokinetics, and tissue inflammation in the case of the optimized formulation. The surface of the optimized RIS microspheres was small and hollow with 134.4 ± 3.5 µm particle size, 1.60 SPAN, 46.7% ± 2.3% implant drug loading, and 93.4% entrapment efficiency. The in-vitro dissolution behavior of RIS-IM had zero-order kinetics and stable blood concentration; no lag time was released for over three months. Furthermore, the RIS-IM was not only non-irritating to tissues but also had good biocompatibility and product stability. Long-acting RIS-IMs with microspheres and film coatings can provide a new avenue for treating schizophrenia.

scholarly journals Photocuring Hyaluronic Acid/Silk Fibroin Hydrogel Containing Curcumin Loaded CHITOSAN Nanoparticles for the Treatment of MG-63 Cells and ME3T3-E1 Cells

Polymers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 2302
Author(s):  
Qingwen Yu ◽  
Zhiyuan Meng ◽  
Yichao Liu ◽  
Zehao Li ◽  
Xing Sun ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Bone Regeneration ◽  
Water Uptake ◽  
Silk Fibroin ◽  
Bone Repair ◽  
Ph Value ◽  
Chitosan Nanoparticles ◽  
Vitro Assay ◽  
Long Term Treatment

After an osteosarcoma excision, recurrence and bone defects are significant challenges for clinicians. In this study, the curcumin (Cur) loaded chitosan (CS) nanoparticles (CCNP) encapsulated silk fibroin (SF)/hyaluronic acid esterified by methacrylate (HAMA) (CCNPs-SF/HAMA) hydrogel for the osteosarcoma therapy and bone regeneration was developed by photocuring and ethanol treatment. The micro or nanofibers networks were observed in the CCNPs-SF/HAMA hydrogel. The FTIR results demonstrated that alcohol vapor treatment caused an increase in β-sheets of SF, resulting in the high compression stress and Young’s modulus of CCNPs-SF/HAMA hydrogel. According to the water uptake analysis, SF caused a slight decrease in water uptake of CCNPs-SF/HAMA hydrogel while CCNPs could enhance the water uptake of it. The swelling kinetic results showed that both the CCNPs and the SF increased the swelling ratio of CCNPs-SF/HAMA hydrogel. The accumulative release profile of CCNPs-SF/HAMA hydrogel showed that the release of Cur from CCNPs-SF/HAMA hydrogel was accelerated when pH value was decreased from 7.4 to 5.5. Besides, compared with CCNPs, the CCNPs-SF/HAMA hydrogel had a more sustainable drug release, which was beneficial for the long-term treatment of osteosarcoma. In vitro assay results indicated that CCNPs-SF/HAMA hydrogel with equivalent Cur concentration of 150 μg/mL possessed both the effect of anti-cancer and promoting the proliferation of osteoblasts. These results suggest that CCNPs-SF/HAMA hydrogel with superior physical properties and the bifunctional osteosarcoma therapy and bone repair may be an excellent candidate for local cancer therapy and bone regeneration.

Hepatic Alveolar Echinococcosis in Cynomolgus Monkeys (Macaca fascicularis)

2004 ◽  
Vol 41 (3) ◽  
pp. 229-234 ◽  
Author(s):  
L. N. Bacciarini ◽  
B. Gottstein ◽  
O. Pagan ◽  
P. Rehmann ◽  
A. Gröne
Keyword(s):  
Macaca Fascicularis ◽  
Alveolar Echinococcosis ◽  
Cynomolgus Monkeys ◽  
Hepatic Alveolar Echinococcosis

scholarly journals Unique MRI findings for differentiation of an early stage of hepatic alveolar echinococcosis

2015 ◽  
Vol 2015 (feb19 1) ◽  
pp. bcr2014208123-bcr2014208123 ◽  
Author(s):  
T. Aoki ◽  
M. Hagiwara ◽  
H. Yabuki ◽  
A. Ito
Keyword(s):  
Alveolar Echinococcosis ◽  
Early Stage ◽  
Mri Findings ◽  
Hepatic Alveolar Echinococcosis

scholarly journals Management of Advanced Hepatic Alveolar Echinococcosis: Report of 42 Cases

2017 ◽  
pp. 16-0557 ◽  
Author(s):  
Bo Qu ◽  
Long Guo ◽  
Guannan Sheng ◽  
Fei Yu ◽  
Guannan Chen ◽  
...  
Keyword(s):  
Alveolar Echinococcosis ◽  
Hepatic Alveolar Echinococcosis

Genome-wide profiling of the expression of serum derived exosomal circRNAs in patients with hepatic alveolar echinococcosis

Gene ◽  
2022 ◽  
pp. 146161
Author(s):  
Selçuk Özdemir ◽  
Nurhak Aksungur ◽  
Necip Altundaş ◽  
Salih Kara ◽  
Ercan Korkut ◽  
...  
Keyword(s):  
Alveolar Echinococcosis ◽  
Hepatic Alveolar Echinococcosis ◽  
Genome Wide

Hepatic Alveolar Echinococcosis

2021 ◽  
Author(s):  
Solange Bresson-Hadni ◽  
Laurent Spahr ◽  
François Chappuis
Keyword(s):  
Access To Care ◽  
Surgical Resection ◽  
Larval Stage ◽  
Echinococcus Multilocularis ◽  
Gold Standard ◽  
Diagnostic Procedure ◽  
Alveolar Echinococcosis ◽  
Opportunistic Infections ◽  
First Line ◽  
Hepatic Alveolar Echinococcosis

AbstractHepatic alveolar echinococcosis (HAE) is a rare but severe zoonosis caused by the pseudotumoral intrahepatic development of the larval stage of the tapeworm Echinococcus multilocularis. HAE is present only in the Northern Hemisphere, predominantly in China. Currently, there is a significant resurgence of cases in historically endemic areas associated with emergence of HAE in countries not previously concerned. Today, in European countries, HAE is often discovered by chance; however, clinicians should be made aware of opportunistic infections that progressively emerged recently as a result of therapeutic or pathological immunosuppression. Ultrasonography is the key first-line diagnostic procedure, with specific serology providing confirmation in 95% of the cases. Albendazole, only parasitostatic, is the mainstay for treatment. Surgical resection, if feasible, is the gold standard for treatment, and more patients are currently eligible for this option because of an earlier diagnosis. The prognosis has considerably improved but remains poor in countries where access to care is less favorable.

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