scholarly journals Clarithromycin-Loaded Poly (Lactic-co-glycolic Acid) (PLGA) Nanoparticles for Oral Administration: Effect of Polymer Molecular Weight and Surface Modification with Chitosan on Formulation, Nanoparticle Characterization and Antibacterial Effects

Polymers ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 1632 ◽  
Author(s):  
A. Alper Öztürk ◽  
Evrim Yenilmez ◽  
Mustafa Güçlü Özarda
Keyword(s):  
Oral Delivery ◽  
Glycolic Acid ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Test Method ◽  
Molecular Weights ◽  
Antibiotic Group ◽  
Surface Modified

Clarithromycin (CLR) is a member of the macrolide antibiotic group. CLR has low systemic oral bioavailability and is a drug of class II of the Biopharmaceutical Classification System. In many studies, using nanoparticles (NPs) as a drug delivery system has been shown to increase the effectiveness and bioavailability of active drug substances. This study describes the development and evaluation of poly (lactic-co-glycolic acid) (PLGA) NPs and chitosan (CS)-coated PLGA NPs for oral delivery of CLR. NPs were obtained by nanoprecipitation technique and characterized in detail, and the effect of three molecular weights (Mw1: 7.000–17.000, Mw2: 38.000–54.000, Mw3: 50.000–190.000) of PLGA and CS coating on particle size (PS), zeta potential (ZP), entrapment efficiency (EE%), and release properties etc. were elucidated. Gastrointestinal stability and cryoprotectant effect tests were performed on the NPs. The PS of the prepared NPs were in the range of 178 to 578 nm and they were affected by the Mw and CS coating. In surface-modified formulations with CS, the ZP of the NPs increased significantly to positive values. EE% varied from 62% to 85%, depending upon the Mw and CS coating. In vitro release studies of CLR-loaded NPs showed an extended release up to 144 h. Peppas–Sahlin and Weibull kinetic model was found to fit best for CLR release from NPs. By the broth microdilution test method, the antibacterial activity of the formulations was determined on Staphylococcus aureus (ATCC 25923), Listeria monocytogenes (ATCC 1911), and Klebsiella pneumoniae (ATCC 700603). The structures of the formulations were clarified by thermal (DSC), FT-IR, and 1H-NMR analysis. The results showed that PS, ZP, EE%, and dissolution rates of NPs were directly related to the Mw of PLGA and CS coating.

scholarly journals Effect of Chitosan Coating on PLGA Nanoparticles for Oral Delivery of Thymoquinone: In Vitro, Ex Vivo, and Cancer Cell Line Assessments

Coatings ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 6
Author(s):  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Md Rizwanullah ◽  
Khalid Umar Fakhri ◽  
Mohd Moshahid Alam Rizvi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Cancer Cell Line ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Cancer Management ◽  
Mcf 7

In the present study, thymoquinone (TQ)-encapsulated chitosan- (CS)-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were formulated using the emulsion evaporation method. NPs were optimized by using 33-QbD approach for improved efficacy against breast cancer. The optimized thymoquinone loaded chitosan coated Poly (d,l-lactide-co-glycolide) nanoparticles (TQ-CS-PLGA-NPs) were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA-MB-231 and MCF-7 cell lines. The surface coating of PLGA-NPs was completed by CS coating and there were no significant changes in particle size and entrapment efficiency (EE) observed. The developed TQ-CS-PLGA-NPs showed particle size, polydispersibility index (PDI), and %EE in the range between 126.03–196.71 nm, 0.118–0.205, and 62.75%–92.17%. The high and prolonged TQ release rate was achieved from TQ-PLGA-NPs and TQ-CS-PLGA-NPs. The optimized TQ-CS-PLGA-NPs showed significantly higher mucoadhesion and intestinal permeation compared to uncoated TQ-PLGA-NPs and TQ suspension. Furthermore, TQ-CS-PLGA-NPs showed statistically enhanced antioxidant potential and cytotoxicity against MDA-MB-231 and MCF-7 cells compared to uncoated TQ-PLGA-NPs and pure TQ. On the basis of the above findings, it may be stated that chitosan-coated TQ-PLGA-NPs represent a great potential for breast cancer management.

scholarly journals BENAZEPRIL HYDROCHLORIDE LOADED NIOSOMAL FORMULATION FOR ORAL DELIVERY: FORMULATION AND CHARACTERIZATION

2018 ◽  
Vol 10 (5) ◽  
pp. 66
Author(s):  
Ameerah A. Radhi
Keyword(s):  
Zeta Potential ◽  
Oral Delivery ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Potential Range ◽  
Transmission Electron ◽  
Study Results ◽  
Span 60 ◽  
A Charge

Objective: The objective of the present study was to formulate niosomal formulations of benazepril hydrochloride in an attempt to overcome the hurdles associated with itʼs poor oral absorption.Methods: Nine formulations were prepared with various ratios of sorbitan monostearate (span 60), sorbitan monopalmitate (span 40) and polyoxyethylene 2 stearyl ether (brij 72) as non-ionic surfactants, cholesterol as a stabilizing agent and soya lecithin as a charge imparting agent. Then, they were characterized for vesicle size, polydispersity (PDI), entrapment efficiency (EE %), release profile, zeta (ζ) potential and transmission electron microscopy (TEM).Results: Niosomal formulations exhibited an efficient entrapment range between (80.4-97.8) percent, vesicles size analyses revealed the formation of homogenously dispersed vesicles having a size range of (3.9±1.7-8.72±4.4) micrometers. The in vitro release studies revealed that all formulations displayed sustained release in comparison with the pure drug. Formulations prepared with span 60 and span 40 possessed adequate stability according to zeta potential analysis, whereas brij 72 failed the test and possessed inadequate zeta potential range. TEM images of the optimized formulations (F7 and F8) have confirmed the formation of vesicles with spherical shapes.Conclusion: Based on the study results, niosomal formulations seem to be attractive alternatives to conventional delivery for benazepril hydrochloride.

scholarly journals Partial Surface Modification of Low Generation Polyamidoamine Dendrimers: Gaining Insight into their Potential for Improved Carboplatin Delivery

Biomolecules ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 214 ◽  
Author(s):  
Nguyen ◽  
Bach ◽  
Nguyen Tran ◽  
Cao ◽  
Nguyen ◽  
...  
Keyword(s):  
Renal Clearance ◽  
Size Range ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Efficient Delivery ◽  
Methoxypolyethylene Glycol ◽  
Potential Applications ◽  
High Entrapment Efficiency ◽  
Surface Modified

Carboplatin (CAR) is a second generation platinum-based compound emerging as one of the most widely used anticancer drugs to treat a variety of tumors. In an attempt to address its dose-limiting toxicity and fast renal clearance, several delivery systems (DDSs) have been developed for CAR. However, unsuitable size range and low loading capacity may limit their potential applications. In this study, PAMAM G3.0 dendrimer was prepared and partially surface modified with methoxypolyethylene glycol (mPEG) for the delivery of CAR. The CAR/PAMAM G3.0@mPEG was successfully obtained with a desirable size range and high entrapment efficiency, improving the limitations of previous CAR-loaded DDSs. Cytocompatibility of PAMAM G3.0@mPEG was also examined, indicating that the system could be safely used. Notably, an in vitro release test and cell viability assays against HeLa, A549, and MCF7 cell lines indicated that CAR/PAMAM G3.0@mPEG could provide a sustained release of CAR while fully retaining its bioactivity to suppress the proliferation of cancer cells. These obtained results provide insights into the potential of PAMAM G3.0@mPEG dendrimer as an efficient delivery system for the delivery of a drug that has strong side effects and fast renal clearance like CAR, which could be a promising approach for cancer treatment.

scholarly journals Ligand Decorated Embelin Loaded PLGA Nanoparticles for Management of Alcohol Induced Hepatotoxicity

2020 ◽  
Vol 10 (1) ◽  
pp. 72-80
Author(s):  
Ajay Kumar ◽  
M. Nikhat Khan ◽  
Jovita Kanoujia ◽  
Amandeep Singh ◽  
Neeraj Mishra
Keyword(s):  
High Performance ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Hep G2 ◽  
Release Studies ◽  
Plga Nanoparticle ◽  
Surface Modified ◽  
Vitro Release

Preparation of surface modified Embelin loaded nanoparticles (GA-PEG-PLGA) for the management of hepatotoxicity. Surface modified Embelin loaded GA-PEG-PLGA NPs were evaluated by NMR, FTIR, TEM techniques and in vitro release studies. The biodistribution of the nanoparticles was assessed by High-performance liquid chromatography (HPLC), and the cellular uptake study was evaluated using Hep G2 cells (liver cells lines). The hepatoprotecttive effect of the surface modified Embelin loaded GA-PEG-PLGA NPs was investigated in-vitro and in-vivo. The surface modified Embelin loaded GA-PEG-PLGA nanoparticles significantly increases the uptake of drug in liver by 2.5 folds more than plain drug. Keywords: Glycyrrhetinic acid, Receptor mediated, Surface functionalization, Embelin, PLGA nanoparticle.

Preparation and Release Profiles of a Solid Oleoylchitosan Coated Poly(lactic-co-glycolic acid) Nanoparticles

2014 ◽  
Vol 936 ◽  
pp. 717-722
Author(s):  
Yan Yan Li ◽  
Feng Song Liu
Keyword(s):  
Drug Release ◽  
Glycolic Acid ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Release Behavior ◽  
Release Rates ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency ◽  
Model Drug

A solid oleoylchitosan (OCS) coated Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (OCS-coated PLGA NPs) were prepared using the emulsification–evaporation method. The nanoparticles in suspension (TEM) and solid state (SEM) were spherical and very regular and compact. The effects of OCS concentration, PLGA concentration, drug concentration, and release media on drug entrapment efficiency and in vitro drug release behavior were investigated for the release properties using rifampicin (RFP) as a model drug. Both the increase of PLGA concentration and the increase of OCS concentration could decrease the drug release rates. The RFP release rates decreased as the RFP concentration increased. The RFP release rate was sensitive to the pH of the release media.

scholarly journals Mangiferin-Loaded Polymeric Nanoparticles: Optical Characterization, Effect of Anti-topoisomerase I, and Cytotoxicity

Cancers ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 1965 ◽  
Author(s):  
Francisco Fabian Razura-Carmona ◽  
Alejandro Pérez-Larios ◽  
Napoleón González-Silva ◽  
Mayra Herrera-Martínez ◽  
Luis Medina-Torres ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Polymeric Nanoparticles ◽  
Biological Activities ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Encapsulation Process ◽  
Mean Size ◽  
High Concentrations

Mangiferin is an important xanthone compound presenting various biological activities. The objective of this study was to develop, characterize physicochemical properties, and evaluate the anti-topoisomerase activity of poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing mangiferin. The nanoparticles were developed by the emulsion solvent evaporation method and the optimal formulation was obtained with a response surface methodology (RSM); this formulation showed a mean size of 176.7 ± 1.021 nm with a 0.153 polydispersibility index (PDI) value, and mangiferin encapsulation efficiency was about 55%. The optimal conditions (6000 rpm, 10 min, and 300 μg of mangiferin) obtained 77% and the highest entrapment efficiency (97%). The in vitro release profile demonstrated a gradual release of mangiferin from 15 to 180 min in acidic conditions (pH 1.5). The fingerprint showed a modification in the maximum absorption wavelength of both the polymer and the mangiferin. Results of anti-toposiomerase assay showed that the optimal formulation (MG4, 25 µg/mL) had antiproliferative activity. High concentrations (2500 µg/mL) of MG4 showed non-in vitro cytotoxic effect on BEAS 2B and HEPG2. Finally, this study showed an encapsulation process with in vitro gastric digestion resistance (1.5 h) and without interfering with the metabolism of healthy cells and their biological activity.

scholarly journals Poly-(Lactic-co-Glycolic) Acid Nanoparticles for Synergistic Delivery of Epirubicin and Paclitaxel to Human Lung Cancer Cells

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4243 ◽  
Author(s):  
Nikita Sharma ◽  
R. Mankamna Kumari ◽  
Nidhi Gupta ◽  
Asad Syed ◽  
Ali H. Bahkali ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Combination Therapy ◽  
Glycolic Acid ◽  
Colloidal Stability ◽  
P53 Protein ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Human Lung Cancer ◽  
Lung Cancer Patients

Combination therapy using chemically distinct drugs has appeared as one of the promising strategies to improve anticancer treatment efficiency. In the present investigation, poly-(lactic-co-glycolic) acid (PLGA) nanoparticles electrostatically conjugated with polyethylenimine (PEI)-based co-delivery system for epirubicin and paclitaxel (PLGA-PEI-EPI-PTX NPs) has been developed. The PLGA-PEI-EPI-PTX NPs exhibited a monodispersed size distribution with an average size of 240.93 ± 12.70 nm as measured through DLS and 70.8–145 nm using AFM. The zeta potential of 41.95 ± 0.65 mV from −17.45 ± 2.15 mV further confirmed the colloidal stability and PEI modification on PLGA nanoparticles. Encapsulation and loading efficiency along with in vitro release of drug for nanoparticles were done spectrophotometrically. The FTIR analysis of PLGA-PEI-EPI-PTX NPs revealed the involvement of amide moiety between polymer PLGA and PEI. The effect of nanoparticles on the cell migration was also corroborated through wound healing assay. The MTT assay demonstrated that PLGA-PEI-EPI-PTX NPs exhibited considerable anticancer potential as compared to the naïve drugs. Further, p53 protein expression analysed through western blot showed enhanced expression. This study suggests that combination therapy using PLGA-PEI-EPI-PTX NPs represent a potential approach and could offer clinical benefits in the future for lung cancer patients.

scholarly journals Bioavailability of Orally Delivered Alpha-Tocopherol by Poly(Lactic-Co-Glycolic) Acid (PLGA) Nanoparticles and Chitosan Covered PLGA Nanoparticles in F344 Rats

10.5772/63305 ◽  
2016 ◽  
Vol 3 ◽  
pp. 8 ◽  
Author(s):  
Lacey C. Simon ◽  
Rhett W. Stout ◽  
Cristina Sabliov
Keyword(s):  
Zeta Potential ◽  
Glycolic Acid ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Particle Systems ◽  
Alpha Tocopherol ◽  
In Vitro Assays ◽  
Pharmacokinetic Studies

It is hypothesized that the bioavailability of αT (alpha-tocopherol), an antioxidant, can be improved when delivered by poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) and chitosan covered PLGA nanoparticles (PLGA-Chi NPs), and that the mucoadhesive properties of chitosan may enhance absorption of αT. PLGA and PLGA-Chi NPs were characterized by measuring entrapment efficiency, size, polydispersity, and zeta potential. Nanoparticle physical stability, chemical stability of entrapped αT, and release kinetics were also measured. Pharmacokinetic studies were conducted by administering PLGA (αT) NPs, PLGA-Chi (αT) NPs, and free αT via oral gavage in rats. The size and zeta potential of the two particle systems were 97.87 ± 2.63 nm and −36.2 ± 1.31 mV for PLGA(αT) NPs, and 134 ± 2.05 nm and 38.0 ± 2.90 mV for PLGA-Chi (αT) nanoparticles in DI water. The particle systems showed to be stable during various in vitro assays. Bioavailability of nanodelivered αT was improved compared to the free αT, by 170% and 121% for PLGA and PLGA-Chi NPs, respectively. It was concluded that while chitosan did not further improved bioavailability of αT, PLGA NPs protected the entrapped drug from the GI environment degradation and proved to be an effective delivery system for αT.

scholarly journals Folate and Borneol Modified Bifunctional Nanoparticles for Enhanced Oral Absorption

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 146 ◽  
Author(s):  
Yifan Yang ◽  
Yunzhi Yin ◽  
Jun Zhang ◽  
Tiantian Zuo ◽  
Xiao Liang ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Oral Absorption ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Oral Drug ◽  
Average Size ◽  
Promising Perspective

Oral delivery is considered the preferred route of administration due to its convenience and favorable compliance. Here, docetaxel (DTX) loaded polylactic-co-glycolic acid (PLGA) nanoparticles, coated with polyethyleneimine–folic acid (PEI-FA) and polyethyleneimine–borneol (PEI-BO), were designed to enhance oral absorption (FA/BO-PLGA-NPs). The FA/BO-PLGA-NPs were spherical and smooth with an average size of (137.0 ± 2.1) nm. Encapsulation efficiency (EE%) and drug loading (DL%) were (80.3 ± 1.8)% and (2.3 ± 0.3)%, respectively. In vitro release studies showed that approximately 62.1% of DTX was released from FA/BO-PLGA-NPs in media at pH 7.4. The reverted gut sac method showed that the absorption of FA/BO-PLGA-NPs in the intestines was approximately 6.0 times that of DTX. Moreover, cellular uptake suggested that the obtained FA/BO-PLGA-NPs could be efficiently internalized into Caco-2 cells via FA-mediated active targeting and BO-mediated P-glycoprotein (P-gp) inhibition. Pharmacokinetics study demonstrated that after oral administration of DTX at a dose of 10 mg/kg in FA/BO-PLGA-NPs, the bioavailability of FA/BO-PLGA-NPs was enhanced by approximately 6.8-fold compared with that of DTX suspension. FA/BO-PLGA-NPs caused no obvious irritation to the intestines. Overall, the FA/BO-PLGA-NP formulation remarkably improved the oral bioavailability of DTX and exhibited a promising perspective in oral drug delivery.

scholarly journals EFFECT OF PEGYLATED EDGE ACTIVATOR ON SPAN 60 BASED- NANOVESICLES: COMPARISON BETWEEN MYRJ 52 AND MYRJ 59

2019 ◽  
Author(s):  
Elsaied H. Elsaied ◽  
Hamdy M Dawaba ◽  
El Sherbini A Ibrahim ◽  
Mohsen I Afouna
Keyword(s):  
Polyethylene Glycol ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Potential Drug ◽  
Span 60 ◽  
Surface Modified ◽  
Vitro Release ◽  
Edge Activator

In recent years, Span 60 based nanovesicles have been the object of growing scientific attention as an alternative potential drug delivery system to conventional liposomes. Surface modification of nanovesicles can adjust the drug release rate and the affinity for the target site. The aim of present work was firstly to study the effects of different PEGylated edge activator (Myrj 52 and Myrj 59) on Span 60 based nanovesicles. Nanovesicles were prepared using Span 60 alone or in combination with Myrj 52 (polyethylene glycol 2000 monostearate) or Myrj 59 (polyethylene glycol 4400 monostearate) by employing the ethanol injection method. Myrj 52and Myrj 59 are hydrophilic nonionic surfactants were used to modify the surface of the developed vesicles. Dynamic light scattering was used to determine the size, zeta potential and polydispersity index of the nanovesicles formulation. The vesicles were also characterized for entrapment efficiency and in vitro release. In current work, the modified nanovesicles size (ranging from 54.32 to 141.7 nm), zeta potential (ranging from -5.67 to -27.1 mV) and polydispersity index (ranging from0.248 to 0.531) indicated that the surface modified nanovesicles vesicles are a homogenous and mono-disperse nanovesicles dispersions. The non-modified nanovesicles are showed higher particles size (>2 times) compared to modified nanovesicles. The modified nanovesicles were showed entrapment efficiency ranging from 36.42 to 78.13 %. All the modified nanovesicles showed accepted in vitro release of TN from nanovesicles (>70% released after 8 h), followed Higuchi models as drug release mechanism. In conclusion, these surface modified nanovesicles could be used as a potential drug carrier for a variety of drugs.

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