Preparation, Evaluation and Bioavailability Studies of Eudragit Coated PLGA Nanoparticles for Sustained Release of Eluxadoline for the Treatment of Irritable Bowel Syndrome

Anwer, Md. Khalid; Al-Shdefat, Ramadan; Ezzeldin, Essam; Alshahrani, Saad; Alshetaili, Abdullah; Iqbal, Muzaffar

doi:10.3389/fphar.2017.00844

Cited by 39 publications

(15 citation statements)

References 22 publications

(26 reference statements)

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“…A sustained release of the drug was observed after 4 h of the study until 48 h in the second phase; it may be due to the lipid and polymer of the NPs, and subsequent immobilization may contribute to the slow release of the drug. The sustained release of the drug ultimately enhanced the bioavailability and, hence, reduced the dose and dosing frequency [38].…”

Section: In-vitro Release Studiesmentioning

confidence: 99%

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

et al. 2020

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Delafloxacin (DFL) is a novel potent and broad-spectrum fluoroquinolone group of antibiotics effective against both Gram-positive and negative aerobic and anaerobic bacteria. In this study, DFL-loaded stearic acid (lipid) chitosan (polymer) hybrid nanoparticles (L-P-NPs) have been developed by single-emulsion-solvent evaporation technique. The mean particle size and polydispersity index (PDI) of optimized DFL-loaded L-P-NPs (F1-F3) were measured in the range of 299–368 nm and 0.215–0.269, respectively. The drug encapsulation efficiency (EE%) and loading capacity (LC%) of DFL-loaded L-P-NPs (F1-F3) were measured in the range of 64.9–80.4% and 1.7–3.8%, respectively. A sustained release of DFL was observed from optimized DFL-loaded L-P-NPs (F3). Minimum inhibitory concentration (MIC) values of the DFL-loaded L-P-NPs (F3) appeared typically to be four-fold lower than those of delafloxacin in the case of Gram-positive strains and was 2-4-fold more potent than those of delafloxacin against Gram-negative strains. The pharmacokinetic study in rats confirmed that the bioavailability (both rate and extent of absorption) of DFL-loaded L-P-NPs was significantly higher (2.3-fold) than the delafloxacin normal suspension. These results concluded that the newly optimized DFL-loaded L-P-NPs were more potent against both Gram-positive and negative strains of bacteria and highly bioavailable in comparison to delafloxacin normal suspension.

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Section: In-vitro Release Studiesmentioning

confidence: 99%

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

et al. 2020

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“… Poly(methacrylic acid)-polysorbate 80-grafted-starch terpolymer and ethylcellulose Diltiazem Enteric delivery and controlled release system 122 35. Pluronic Efavirenz Microfold cells (M-cells) targeted delivery system 123 36. Poly(D,L-lactide-co-glycolide) and Eudragit S100 Eluxadoline Enteric delivery and sustained release system 124 37.…”

Section: Enteric-coated Nanoparticle Formulations For Non-colorectal mentioning

confidence: 99%

<p>Enteric-Coated Strategies in Colorectal Cancer Nanoparticle Drug Delivery System</p>

Wathoni

Nguyen

Rusdin

et al. 2020

DDDT

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Colorectal cancer is one of the most common cancer diseases with the increase of cases prevalence >5% every year. Multidrug resistance mechanisms and non-localized therapy become primary problems of chemotherapy drugs for curing colorectal cancer disease. Therefore, the enteric-coated nanoparticle system has been studied and proved to be able to resolve those problems with good performance for colorectal cancer. The highlight of our review aims to summarize and discuss the enteric-coated nanoparticle drug delivery system specific for colorectal cancer disease. The main and supporting literatures were collected from published research articles of journals indexed in Scopus and PubMed databases. In the oral route of administration, Eudragit pH-sensitive copolymer as a coating agent prevents the degradation of the nanoparticle system from the gastric fluid and releases drug to intestinal-colon track. Therefore, it provides a colon-specific targeting ability. Impressively, enteric-coated nanoparticles having a sustained release profile significantly increase the cytotoxic effect of chemotherapeutic drugs and achieve cell-specific target delivery. The enteric-coated nanoparticle drug delivery system represents an excellent modification to improve the effectiveness and performance of anticancer drugs for colorectal cancer disease in terms of the oral route of administration.

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“…[13][14][15] The sustained release time of PLGA NPs can be programmed by optimizing particle, size, morphology, and molecular weight of PLGA. 16 A few drug-delivery systems such as topical preparation, 17,18 extended release tablets, 9 and nail lacquers 19 with APM have been investigated in order to enhance its in vitro dissolution rate, efficacy, PK profile, and in vivo bioavailability. To the best knowledge of the authors, PLGA polymeric nanoparticles of APM have not yet been investigated in literature despite several favorable characteristics of the latter for nanoparticle preparation including poor water solubility, low bioavailability, and prominent adverse effects.…”

Section: Introductionmentioning

confidence: 99%

<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

Anwer

Mohammad

Ezzeldin

et al. 2019

IJN

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120

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Background Apremilast (APM) is a novel, orally administered small molecule drug approved for treatment of psoriasis or psoriatic arthritis. Due to its low solubility and permeability, it is classified as a class IV drug according to BCS classification. Dose titration is recommended during APM treatment due to its tolerability and twice-daily dosing regimen issues. Materials and Methods In this study, three different APM-loaded PLGA nanoparticles (F1–F3) were prepared by single emulsion and evaporation method. Based on particle size, PDI, zeta potential (ZP), entrapment efficiency (%EE), drug loading (%DL), and spectral characterization, the nanoparticles (F3) were optimized. The F3 nanoparticles were further evaluated for in vitro release and in vivo pharmacokinetic studies in rats. Results The optimized nanoparticles (F3) had particles size 307.3±8.5 nm with a low PDI value 0.317, ZP of −43.4±2.6 mV, EE of 61.1±1.9% and DL of 1.9±0.1%. The in vitro release profile showed a sustained release pattern of F3 nanoparticles of APM. The pharmacokinetic results showed 2.25 times increase in bio-availability of F3 nanoparticles compared to normal APM suspension. Moreover, significant increase in half-life and mean residence time confirms long-term retention of F3 nanoparticles. Conclusion Bioavailability enhancement along-with long-term retention of the APM-loaded PLGA nanoparticles might be helpful for the once-daily regimen treatment.

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Preparation, Evaluation and Bioavailability Studies of Eudragit Coated PLGA Nanoparticles for Sustained Release of Eluxadoline for the Treatment of Irritable Bowel Syndrome

Cited by 39 publications

References 22 publications

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

<p>Enteric-Coated Strategies in Colorectal Cancer Nanoparticle Drug Delivery System</p>

<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

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