scholarly journals Chitosan-Coated PLGA Nanoparticles for Enhanced Ocular Anti-Inflammatory Efficacy of Atorvastatin Calcium

2020 ◽  
Vol Volume 15 ◽  
pp. 1335-1347 ◽  
Author(s):  
Mona G Arafa ◽  
Germeen NS Girgis ◽  
Marwa S El-Dahan
Keyword(s):  
Plga Nanoparticles ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Formulation and Evaluation of Atorvastatin Calcium-Poly-ε-Caprolactone Nanoparticles Loaded Ocular Inserts for Sustained Release and Antiinflammatory Efficacy

2020 ◽  
Vol 21 (15) ◽  
pp. 1688-1698
Author(s):  
Germeen N.S. Girgis
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Average Weight ◽  
Drug Release Profile ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Purpose: The work was performed to investigate the feasibility of preparing ocular inserts loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system. Methods: First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with free drug-loaded ocuserts. Results: The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and 62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to 0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability, ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant lowering in PMN count after 3h. Conclusion: These findings proposed a possibly simple, new and affordable price technique to prepare promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory efficacy.

scholarly journals Correction to: Cholesterol-functionalized carvedilol-loaded PLGA nanoparticles: anti-inflammatory, antioxidant, and antitumor effects

2020 ◽  
Vol 22 (7) ◽  
Author(s):  
Ana Luiza C. de S. L. Oliveira ◽  
Alaine M. dos Santos-Silva ◽  
Arnóbio A. da Silva-Júnior ◽  
Vinícius B. Garcia ◽  
Aurigena A. de Araújo ◽  
...  
Keyword(s):  
Plga Nanoparticles ◽  
Antitumor Effects ◽  
Anti Inflammatory

MRI-assessed therapeutic effects of locally administered PLGA nanoparticles loaded with anti-inflammatory siRNA in a murine arthritis model

2012 ◽  
Vol 161 (3) ◽  
pp. 772-780 ◽  
Author(s):  
Bernard C.M. te Boekhorst ◽  
Linda B. Jensen ◽  
Stefano Colombo ◽  
Amir K. Varkouhi ◽  
Raymond M. Schiffelers ◽  
...  
Keyword(s):  
Plga Nanoparticles ◽  
Therapeutic Effects ◽  
Arthritis Model ◽  
Anti Inflammatory

scholarly journals A Novel Sustained Anti-Inflammatory Effect of Atorvastatin—Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1658
Author(s):  
Dalia H. Abdelkader ◽  
Ahmed Kh. Abosalha ◽  
Mohamed A. Khattab ◽  
Basmah N. Aldosari ◽  
Alanood S. Almurshedi
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
In Vitro Release ◽  
In Vivo Evaluation ◽  
Water Emulsion ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.

scholarly journals Preparation of Biodegradable PLGA-Nanoparticles Used for pH-Sensitive Intracellular Delivery of an Anti-inflammatory Bacterial Toxin to Macrophages

2020 ◽  
Vol 68 (4) ◽  
pp. 363-368
Author(s):  
Ayaka Harada ◽  
Hiroyasu Tsutsuki ◽  
Tianli Zhang ◽  
Ruda Lee ◽  
Kinnosuke Yahiro ◽  
...  
Keyword(s):  
Intracellular Delivery ◽  
Plga Nanoparticles ◽  
Ph Sensitive ◽  
Bacterial Toxin ◽  
Anti Inflammatory

scholarly journals Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity

2020 ◽  
Author(s):  
Blerina Shkodra-Pula ◽  
Christian Kretzer ◽  
Paul M. Jordan ◽  
Paul Klemm ◽  
Andreas Koeberle ◽  
...  
Keyword(s):  
Product Formation ◽  
Plga Nanoparticles ◽  
Drug Uptake ◽  
Hydrodynamic Diameter ◽  
Prostaglandin E ◽  
Intact Cells ◽  
Vis Spectroscopy ◽  
Nanoprecipitation Method ◽  
Anti Inflammatory ◽  
Human Polymorphonuclear Leukocytes

Abstract Background: Dual inhibitors of the 5-lipoxygenase-activating protein (FLAP) and the microsomal prostaglandin E2 synthase-1 (mPGES-1) may exert better anti-inflammatory efficacy and lower risks of adverse effects versus non-steroidal anti-inflammatory drugs. Despite these advantages, many dual FLAP/mPGES-1 inhibitors are acidic lipophilic molecules with low solubility and strong tendency for plasma protein binding that limit their bioavailability and bioactivity. Here, we present the encapsulation of the dual FLAP/mPGES-1 inhibitor BRP-187 into the biocompatible polymers acetalated dextran (Acdex) and poly(lactic-co-glycolic acid) (PLGA) via nanoprecipitation. Results: The nanoparticles containing BRP-187 were prepared by the nanoprecipitation method and analyzed by dynamic light scattering regarding their hydrodynamic diameter, by scanning electron microscopy for morphology properties, and by UV-VIS spectroscopy for determination of the encapsulation efficiency of the drug. Moreover, we designed fluorescent BRP-187 particles, which showed high cellular uptake by leukocytes, as analyzed by flow cytometry. Finally, BRP-187 nanoparticles were tested in human polymorphonuclear leukocytes and macrophages to determine drug uptake, cytotoxicity, and efficiency to inhibit FLAP and mPGES-1.Conclusion: Our results demonstrate that encapsulation of BRP-187 into Acdex and PLGA is feasible, and both PLGA- and Acdex-based particles loaded with BRP-187 are more efficient in suppressing 5-lipooxygenase product formation and prostaglandin E2 biosynthesis in intact cells as compared to the free compound, particularly after prolonged preincubation periods.

scholarly journals Evaluating the Mucoprotective Effects of Glycyrrhizic Acid Loaded Polymeric Nanoparticles Against 5-Fluorouracil Induced Intestinal Mucositis in Murine Model via Suppression of Inflammatory Mediators and Oxidative Stress

2021 ◽  
Author(s):  
Mahira Zeeshan ◽  
Ayesha Atiq ◽  
Qurat Ul Ain ◽  
Jawad Ali ◽  
Salman Khan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Inflammatory Mediators ◽  
Glycyrrhizic Acid ◽  
Plga Nanoparticles ◽  
Therapeutic Effects ◽  
Therapeutic Action ◽  
Polymeric Nanocarriers ◽  
Intestinal Mucositis ◽  
Anti Inflammatory

Abstract Objectives: 5-Flourouracil (5-FU), a chemotherapeutic drug, is linked with severe deteriorating effects on intestine leading to mucositis. Further, Glycyrrhizic acid is a renown herbal medicine with combined mucoprotective, antioxidant and anti-inflammatory actions, however associated with pharmacokinetics limitations. Owing to its remarkable therapeutic action in inflammatory bowel disease inside the polymeric nanocarriers, we have tried to explore its activity against 5-FU led intestinal mucositis. Polymeric nanocarriers proved to be efficient drug delivery vehicles for long-term remedy against inflammatory diseases, however, yet not explored for 5-FU induced mucositis. Therefore, the study aimed to produce Glycyrrhizic acid loaded poly lactic-co-glycolic acid (GA-PLGA) nanoparticles to evaluate its protective and therapeutic effects on intestinal mucosa against 5-FU mediated mucositis. Methods: For the said purpose, GA-PLGA nanoparticles were prepared using modified double emulsion method, physicochemically characterized and tested for invitro drug release. Thereafter, mucositis was induced by 5-FU (50 mg/kg; IP) administration to the mice for the first three days (day 0, 1, 2) and orally treated with GA-PLGA nanoparticles till seventh day (day 0-6). Results: GA-PLGA nanoparticles significantly reduced mucositis severity as manifested through recovered body weight, diarrhea score, distress, and anorexia. Further, 5-FU induced intestinal histopathological damage, altered villi-crypt length, low goblet cell count, elevated pro-inflammatory mediators and suppressed antioxidant enzymes were reversed by GA-PLGA nanoparticles’ sustained release therapeutic action. Conclusion: Morphological, behavioral, histological, and biochemical results suggested that GA-PLGA nanoparticles found to be efficient, biocompatible, targeted, sustained release drug delivery nano-vehicle for enhanced mucoprotective, anti-inflammatory and antioxidant effects in ameliorating 5-FU intestine mucositis.

scholarly journals Ex Vivo Permeation of Carprofen Vehiculated by PLGA Nanoparticles through Porcine Mucous Membranes and Ophthalmic Tissues

Nanomaterials ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 355 ◽  
Author(s):  
Lídia Gómez-Segura ◽  
Alexander Parra ◽  
Ana Cristina Calpena-Campmany ◽  
Álvaro Gimeno ◽  
Immaculada Gómez de Aranda ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Cell Structure ◽  
Topical Administration ◽  
Plga Nanoparticles ◽  
In Vivo Studies ◽  
Ex Vivo Permeation ◽  
Mucous Membranes ◽  
Anti Inflammatory ◽  
Almost All

(1) Background: Carprofen (CP), 2-(6-chlorocarbazole) propionic acid, is used as an anti-inflammatory, analgesic and anti-pyretic agent and it belongs to the family of non-steroidal anti-inflammatory drugs (NSAIDs). CP has some adverse reactions in systemic administration; for this reason, topical administration with CP nanoparticles (CP-NPs) can be an optimal alternative. The main objective of this work is the investigation of ex vivo permeation of CP through different types of porcine mucous membranes (buccal, sublingual and vaginal) and ophthalmic tissues (cornea, sclera and conjunctiva) to compare the influence of CP-NPs formulation over a CP solution (CP-Solution). (2) Methods: The ex vivo permeation profiles were evaluated using Franz diffusion cells. Furthermore, in vivo studies were performed to verify that the formulations did not affect the cell structure and to establish the amount retained (Qr) in the tissues. (3) Results: Permeation of CP-NPs is more effective in terms of drug retention in almost all tissues (with the exception of sclera and sublingual). In vivo studies show that neither of the two formulations affects tissue structure, so both formulations are safe. (4) Conclusions: It was concluded that CP-NPs may be a useful tool for the topical treatment of local inflammation in veterinary and human medicine.

scholarly journals Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity

2020 ◽  
Author(s):  
Blerina Shkodra-Pula ◽  
Christian Kretzer ◽  
Paul M. Jordan ◽  
Paul Klemm ◽  
Andreas Koeberle ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Product Formation ◽  
Plga Nanoparticles ◽  
Drug Uptake ◽  
Hydrodynamic Diameter ◽  
Intact Cells ◽  
Vis Spectroscopy ◽  
Nanoprecipitation Method ◽  
Anti Inflammatory ◽  
Human Polymorphonuclear Leukocytes

Abstract Background: Dual inhibitors of the 5-lipoxygenase-activating protein (FLAP) and the microsomal prostaglandin E2 synthase-1 (mPGES-1) may exert better anti-inflammatory efficacy and lower risks of adverse effects versus non-steroidal anti-inflammatory drugs. Despite these advantages, many dual FLAP/mPGES-1 inhibitors are acidic lipophilic molecules with low solubility and strong tendency for plasma protein binding that limit their bioavailability and bioactivity. Here, we present the encapsulation of the dual FLAP/mPGES-1 inhibitor BRP-187 into the biocompatible polymers acetalated dextran (Acdex) and poly(lactic-co-glycolic acid) (PLGA) via nanoprecipitation. Results: The nanoparticles containing BRP-187 were prepared by the nanoprecipitation method and analyzed by dynamic light scattering regarding their hydrodynamic diameter, by scanning electron microscopy for morphology properties, and by UV-VIS spectroscopy for determination of the encapsulation efficiency of the drug. Moreover, we designed fluorescent BRP-187 particles, which showed high cellular uptake by leukocytes, as analyzed by flow cytometry. Finally, BRP-187 nanoparticles were tested in human polymorphonuclear leukocytes and macrophages to determine drug uptake, cytotoxicity, and efficiency to inhibit FLAP and mPGES-1.Conclusion: Our results demonstrate that encapsulation of BRP-187 into Acdex and PLGA is feasible, and both PLGA- and Acdex-based particles loaded with BRP-187 are more efficient in suppressing 5-lipooxygenase product formation and prostaglandin E2 biosynthesis in intact cells as compared to the free compound, particularly after prolonged preincubation periods.

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