scholarly journals Electrospinning Preparation of Timosaponin B-II-Loaded PLLA Nanofibers and Their Antitumor Recurrence Activities In Vivo

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Zhonghua Huo ◽  
Yan Qiu ◽  
Zhuling Chu ◽  
Peng Yin ◽  
Wenquan Lu ◽  
...  
Keyword(s):  
Drug Carrier ◽  
Amorphous State ◽  
Water Soluble ◽  
Sustained Delivery ◽  
Water Soluble Drug ◽  
Release Studies ◽  
Long Time ◽  
Model Drug

Poly(L-lactic)-acid (PLLA) as a drug carrier and a water-soluble drug timosaponin B-II (TB-II) as a model drug were selected to prepare drug-loaded nanofibers by electrospinning. The average diameters of pure PLLA nanofibers and TB-II-loaded nanofibers were 212.5 ± 68.5, 219.7 ± 57.8, 232.8 ± 66.9, and 232.9 ± 97.7 nm, respectively. DSC and XRD results demonstrated that TB-II was well incorporated into the nanofibers in an amorphous state. FI-TR spectroscopy indicated that TB-II had good compatibility with PLLA. In vitro release studies showed that TB-II was rapidly released from the nanofibers within 6 h, followed by a gradual release for long time. In vivo biosafety test revealed no noticeable toxicity of these TB-II nanofibers. The TB-II released from the nanofibers had obvious inhibition effect against human hepatocellular carcinoma SMMC 7721 cells both in vivo and in vitro. It was confirmed that the TB-II-loaded nanofibers were a sustained delivery system which could effectively inhibit the tumor growth and recurrence after surgery.

scholarly journals Synthesis, Degradation, Biocompatibility and Drug Release Studies of Bis 2-Hydroxy Ethyl Terephthalate-based Poly(Mannitol-Citric-Sebacate) Ester

2016 ◽  
Vol 1 (1) ◽  
pp. 9-16
Author(s):  
Athira K Sunil ◽  
Sarkar K ◽  
Kaushik Chatterjee
Keyword(s):  
Drug Release ◽  
Drug Carrier ◽  
Condensation Process ◽  
Burst Release ◽  
Release Studies ◽  
Biodegradable Poly ◽  
Model Drug ◽  
Melt Condensation

Bis 2-Hydroxy Ethyl Terephthalate-based biodegradable poly(mannitol-citric-sebacate) has been synthesized by catalyst-free melt condensation process using two different diacids and Bis 2-Hydroxy Ethyl Terephthalate with D-mannitol as monomers having a potential to be metabolized in vivo. The biocompatibility of the polymer, Bis 2-Hydroxy Ethyl Terephthalate-poly(mannitol-citric-sebacate) has been tested using human primary stromal cells. In vitro degradation of Bis 2-Hydroxy Ethyl Terephthalate-poly(mannitol-citric-sebacate) polymer in Phosphate Buffered Saline solution carried out at physiological conditions indicates that the degradation goes to completion after 23 days. The usage of Bis 2-Hydroxy Ethyl Terephthalate-poly(mannitol-citric-sebacate) polymer as a drug carrier has been analyzed by doping the polymer with Doxorubicin model drug and the release rate has been studied by mass loss over time. The cumulative drug-release profiles exhibit a biphasic release with an initial burst release and cumulative 100 percent release within 14 days.

scholarly journals Improved Bioavailability of Poorly Water-Soluble Drug by Targeting Increased Absorption through Solubility Enhancement and Precipitation Inhibition

2021 ◽  
Vol 14 (12) ◽  
pp. 1255
Author(s):  
Ju-Hyun Lee ◽  
Chulhun Park ◽  
Kwon-Yeon Weon ◽  
Chin-Yang Kang ◽  
Beom-Jin Lee ◽  
...  
Keyword(s):  
Drug Release ◽  
Amorphous State ◽  
Water Soluble ◽  
Pharmacokinetic Data ◽  
In Vivo Test ◽  
Water Soluble Drug ◽  
Absorption Area ◽  
Poorly Water Soluble

Itraconazole (ITZ) is a class II drug according to the biopharmaceutical classification system. Its solubility is pH 3-dependent, and it is poorly water-soluble. Its pKa is 3.7, which makes it a weak base drug. The aim of this study was to prepare solid dispersion (SD) pellets to enhance the release of ITZ into the gastrointestinal environment using hot-melt extrusion (HME) technology and a pelletizer. The pellets were then filled into capsules and evaluated in vitro and in vivo. The ITZ changed from a crystalline state to an amorphous state during the HME process, as determined using DSC and PXRD. In addition, its release into the gastrointestinal tract was enhanced, as was the level of ITZ recrystallization, which was lower than the marketed drug (Sporanox®), as assessed using an in vitro method. In the in vivo study that was carried out in rats, the AUC0–48h of the commercial formulation, Sporanox®, was 1073.9 ± 314.7 ng·h·mL−1, and the bioavailability of the SD pellet (2969.7 ± 720.6 ng·h·mL−1) was three-fold higher than that of Sporanox® (*** p < 0.001). The results of the in vivo test in beagle dogs revealed that the AUC0–24h of the SD-1 pellet (which was designed to enhance drug release into gastric fluids) was 3.37 ± 3.28 μg·h·mL−1 and that of the SD-2 pellet (which was designed to enhance drug release in intestinal fluids) was 7.50 ± 4.50 μg·h·mL−1. The AUC of the SD-2 pellet was 2.2 times higher than that of the SD-1 pellet. Based on pharmacokinetic data, ITZ would exist in a supersaturated state in the area of drug absorption. These results indicated that the absorption area is critical for improving the bioavailability of ITZ. Consequently, the bioavailability of ITZ could be improved by inhibiting precipitation in the absorption area.

scholarly journals Fabrication of Quaternized Chitosan Nanoparticles Using Tripolyphosphate/Genipin Dual Cross-Linkers as a Protein Delivery System

Polymers ◽  
2018 ◽  
Vol 10 (11) ◽  
pp. 1226 ◽  
Author(s):  
Kuo-Yu Chen ◽  
Si-Ying Zeng
Keyword(s):  
Protein Delivery ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
Weight Ratio ◽  
Water Soluble ◽  
Trimethylammonium Chloride ◽  
Sustained Delivery ◽  
Release Studies ◽  
Predicted Values

Various amounts of 2-((acryloyloxy)ethyl)trimethylammonium chloride were grafted onto chitosan (CS) via redox polymerization method to obtain water-soluble quaternized CS (QCS). The QCS nanoparticles loaded with bovine serum albumin (BSA) were then produced by ionic gelation with tripolyphosphate (TPP) and further covalently cross-linked with genipin. The formation of QCS nanoparticles was optimized as a function of monomer grafting yield, QCS/TPP weight ratio, and QCS/genipin weight ratio by Box-Behnken design and response surface methodology. The results showed that QCS nanoparticles prepared with a grafting yield of 50%, QCS/TPP weight ratio of 7.67, and QCS/genipin weight ratio of 60 had a particle size of 193.68 ± 44.92 nm, polydispersity of 0.232, zeta potential of +23.97 mV and BSA encapsulation efficiency of 46.37 ± 2.89%, which were close to the predicted values from mathematical models. In vitro drug release studies at pH 1.2 and pH 7.4 exhibited that the release rate of BSA was significantly decreased and the release period was significantly prolonged after QCS nanoparticles cross-linking with genipin. Therefore, QCS nanoparticles cross-linked with TPP/genipin dual cross-linkers may be a promising protein drug carrier for a prolonged and sustained delivery.

AMORPHOUS SOLID DISPERSIONS OF PIOGLITAZONE HYDROCHLORIDE USING CREMOPHOR RH 40 AND POLOXAMER 188: IN VITRO AND IN VIVO EVALUATION

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (01) ◽  
pp. 45-55
Author(s):  
R. P Swain ◽  
B. B Subudhi ◽  
Keyword(s):  
Solid Dispersions ◽  
Amorphous State ◽  
Amorphous Solid ◽  
Water Soluble ◽  
Amorphous Solid Dispersions ◽  
In Vivo Evaluation ◽  
In Vivo Test ◽  
Water Soluble Drug

The study was aimed to improve dissolution and bioavailability of developed stable amorphous solid dispersions (SDs) of pioglitazone hydrochloride (PGH), a poorly water soluble drug. TGA showed compatibility with the polymers. The significant change in melting pattern of the PGH observed in the DSC thermograms supported by XRD patterns and SEM indicated change from crystalline to amorphous state. Prevention of recrystallization during storage suggested stability of formulation. Cremophor RH 40 based SD (solvent method) remarkably increased the dissolution within 15 min and was supported by dissolution parameters (Q15, IDR, RDR, % DE, f1, f2). In vivo test showed significantly (p < 0.05) higher AUC0-t and Cmax, which were about 4.46 and 4.84 times that of pure drug, respectively. Cremophor RH 40 was found to be a suitable carrier for SM for preparation of SDs of PH as evident from increased dissolution and bioavailability.

scholarly journals Folate-Functionalized Mesoporous Hollow SnO2 Nanofibers as a Targeting Drug Carrier to Improve the Antitumor Effect of Paclitaxel for Liver Cancer Therapy

2018 ◽  
Vol 2018 ◽  
pp. 1-11
Author(s):  
Huiling Lv ◽  
Chao Wu ◽  
Xuan Liu ◽  
Andi Bai ◽  
Yue Cao ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Liver Cancer ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Hollow Structure ◽  
Amorphous State ◽  
Outer Diameter ◽  
Drug Delivery Carrier

In this study, we prepared PTX-loaded mesoporous hollow SnO2 nanofibers conjugated with folic acid (SFNFP) for liver cancer therapy. According to SEM and TEM characterization, SFNF showed a mesoporous hollow structure. The average outer diameter was 200 nm, and the wall thickness was 50 nm. The DSC and XRD study showed that PTX in the channels of nanofibers was present in an amorphous state. The in vitro release experiments demonstrated that SFNF could efficiently improve the dissolution rate of PTX. Both in vitro cell experiments and in vivo antitumor experiments showed that SFNFP could efficiently inhibit the growth of liver cancer cells. Therefore, SFNF is a promising targeting antitumor drug delivery carrier.

scholarly journals FORMULATION OF NANOPARTICLES OF TELMISARTAN INCORPORATED IN CARBOXYMETHYLCHITOSAN FOR THE BETTER DRUG DELIVERY AND ENHANCED BIOAVAILABILITY

2017 ◽  
Vol 10 (9) ◽  
pp. 236
Author(s):  
Upasana Yadav ◽  
Angshuman Ray Chowdhuri ◽  
Sumanta Kumar Sahu ◽  
Nuzhat Husain ◽  
Qamar Rehman
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Water Soluble ◽  
Bioavailability Enhancement ◽  
Water Soluble Drug ◽  
Efficient Option

  Objective: In this study, we have made an attempt to the developed formulation of nanoparticles (NPs) of telmisartan (TLM) incorporated in carboxymethyl chitosan (CMCS) for the better drug delivery and enhanced bioavailability.Materials and Methods: The NPs size and morphology were investigated by high-resolution transmission electron microscopy and field emission scanning electron microscopy, respectively. The crystal structures and surface functional groups were analyzed using X-ray diffraction pattern, and Fourier transform infrared spectroscopy, respectively.Results: To increase the solubility of TLM by targeted delivery of the drug through polymeric NPs is an alternative efficient, option for increasing the solubility. TLM nanosuspension powders were successfully formulated for dissolution and bioavailability enhancement of the drug. We focused on evaluating the influence of particle size and crystalline state on the in vitro and in vivo performance of TLM.Conclusion: In summary, we have developed a new approach toward the delivery of poorly water-soluble drug TLM by CMCS NPs. The particles having a good drug loading content and drug encapsulation efficiency. The cytotoxicity of the synthesized NPs is also very less.

In Vitro-In Vivo Correlation for Solid Dispersion of a Poorly Water-Soluble Drug Efonidipine Hydrochloride

2020 ◽  
Vol 21 (5) ◽  
Author(s):  
Xu Cheng ◽  
Jianlong Gao ◽  
Jiaqi Li ◽  
Gang Cheng ◽  
Meijuan Zou ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug
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