Formulation and ex vivo evaluation of polymeric nanoparticles for controlled delivery of corticosteroids to the skin and the corneal epithelium

2017 ◽  
Vol 115 ◽  
pp. 122-130 ◽  
Author(s):  
Benjamin Balzus ◽  
Fitsum Feleke Sahle ◽  
Stefan Hönzke ◽  
Christian Gerecke ◽  
Fabian Schumacher ◽  
...  
Keyword(s):  
Corneal Epithelium ◽  
Ex Vivo ◽  
Polymeric Nanoparticles ◽  
Controlled Delivery

scholarly journals Controlled Delivery of BET-PROTACs: In Vitro Evaluation of MZ1-Loaded Polymeric Antibody Conjugated Nanoparticles in Breast Cancer

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 986
Author(s):  
Francisco J. Cimas ◽  
Enrique Niza ◽  
Alberto Juan ◽  
María del Mar Noblejas-López ◽  
Iván Bravo ◽  
...  
Keyword(s):  
Polymeric Nanoparticles ◽  
Controlled Delivery ◽  
New Family ◽  
Bet Inhibitors ◽  
Release Studies ◽  
Bromodomain Proteins ◽  
Therapeutic Properties ◽  
Tumoral Cells ◽  
Efficacy Profile

Bromo and extraterminal domain (BET) inhibitors-PROteolysis TArgeting Chimera (BETi-PROTAC) is a new family of compounds that induce proteasomal degradation through the ubiquitination of the tagged to BET inhibitors Bromodomain proteins, BRD2 and BRD. The encapsulation and controlled release of BET-PROTACs through their vectorization with antibodies, like trastuzumab, could facilitate their pharmacokinetic and efficacy profile. Antibody conjugated nanoparticles (ACNPs) using PROTACs have not been designed and evaluated. In this pioneer approach, the commercial MZ1 PROTAC was encapsulated into the FDA-approved polymeric nanoparticles. The nanoparticles were conjugated with trastuzumab to guide the delivery of MZ1 to breast tumoral cells that overexpress HER2. These ACNPs were characterized by means of size, polydispersity index, and Z-potential. Morphology of the nanoparticles, along with stability and release studies, completed the characterization. MZ1-loaded ACNPs showed a significant cytotoxic effect maintaining its mechanism of action and improving its therapeutic properties.

scholarly journals ID3024 Polymeric nanoparticles display bactericidal effect and selective fermentation for the treatment of acne vulgaris

2017 ◽  
Vol 4 (S) ◽  
pp. 34
Author(s):  
Ming-Fa Hsieh
Keyword(s):  
Human Skin ◽  
Ex Vivo ◽  
Polymeric Nanoparticles ◽  
Acne Vulgaris ◽  
Short Chain Fatty Acids ◽  
Bactericidal Effect ◽  
Skin Microbiome ◽  
Poly Ethylene Glycol ◽  
Effective Doses ◽  
Poly Ethylene

The use of antibiotics in the treatment of acne in specific group (pregnant women) of patients can lead to serious complications. We have previously demonstrated that the nanoparticles made of block copolymers of poly (ethylene glycol) and poly(e-caprolactone) can inhibit the growth of Propionibacterium acnes (P. acnes), a bacterium highly associated with the progress of acne vulgaris in the human skin [Polymers 2016; 8, 321]. To reduce the amount of antibiotics used in the treatment of skin acne, we have further demonstrated that a bacterium in the human skin microbiome can utilize PEG-based polymers to produce various short-chain fatty acids (SCFAs) which suppressed the growth of P. acnes. PEG-based polymers were chosen as selective fermentation initiators which specifically induced the fermentation of the skin commensal bacterium but not P. acnes. Interestingly, PEG-based polymers can efficiently suppress the growth of P. acnes. An acne ex vivo explant was established by using acne biopsies collected from patients with acne vulgaris at the early and middle stages. The levels of pro-inflammatory interleukin (IL)-8 cytokine in early- and middle-staged acnes were significantly higher than those in healthy skins. Incubation of acne ex vivo explants with sucrose remarkably reduced the level of IL-8 and the number of P. acnes. Results from mouse studies revealed that PEG-based polymer functions as antibiotic adjuvants which can considerably reduce the effective doses of clindamycin, a clinically-used acne antibiotic

Polymeric nanoparticles as carrier for targeted and controlled delivery of anticancer agents

2019 ◽  
Vol 10 (8) ◽  
pp. 527-550 ◽  
Author(s):  
Vahid Taghipour-Sabzevar ◽  
Tahere Sharifi ◽  
Mehrdad Moosazadeh Moghaddam
Keyword(s):  
Adverse Effect ◽  
Drug Delivery ◽  
Controlled Release ◽  
Anticancer Agents ◽  
Blood Circulation ◽  
Enzymatic Degradation ◽  
Water Solubility ◽  
Polymeric Nanoparticles ◽  
Controlled Delivery ◽  
Drug Adverse Effect

In recent decades, many novel methods by using nanoparticles (NPs) have been investigated for diagnosis, drug delivery and treatment of cancer. Accordingly, the potential of NPs as carriers is very significant for the delivery of anticancer drugs, because cancer treatment with NPs has led to the improvement of some of the drug delivery limitations such as low blood circulation time and bioavailability, lack of water solubility, drug adverse effect. In addition, the NPs protect drugs against enzymatic degradation and can lead to the targeted and/or controlled release of the drug. The present review focuses on the potential of NPs that can help the targeted and/or controlled delivery of anticancer agents for cancer therapy.

scholarly journals Polymeric nanoparticles based topical gel of poorly soluble drug: Formulation, ex-vivo and in vivo evaluation

2017 ◽  
Vol 6 (2) ◽  
pp. 184-191 ◽  
Author(s):  
Mohammed Elmowafy ◽  
Ahmed Samy ◽  
Abdelaziz E. Abdelaziz ◽  
Khaled Shalaby ◽  
Ayman Salama ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Polymeric Nanoparticles ◽  
Drug Formulation ◽  
In Vivo Evaluation ◽  
Topical Gel ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

scholarly journals How Can Biomolecules Improve Mucoadhesion of Oral Insulin? A Comprehensive Insight using Ex-Vivo, In Silico, and In Vivo Models

Biomolecules ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 675 ◽  
Author(s):  
Mariana Amaral ◽  
Ana Sofia Martins ◽  
José Catarino ◽  
Pedro Faísca ◽  
Pradeep Kumar ◽  
...  
Keyword(s):  
In Silico ◽  
Ex Vivo ◽  
Polymeric Nanoparticles ◽  
Spherical Shape ◽  
Diabetic Rats ◽  
Laser Scattering ◽  
In Vivo Models ◽  
Mean Size

Currently, insulin can only be administered through the subcutaneous route. Due to the flaws associated with this route, it is of interest to orally deliver this drug. However, insulin delivered orally has several barriers to overcome as it is degraded by the stomach’s low pH, enzymatic content, and poor absorption in the gastrointestinal tract. Polymers with marine source like chitosan are commonly used in nanotechnology and drug delivery due to their biocompatibility and special features. This work focuses on the preparation and characterization of mucoadhesive insulin-loaded polymeric nanoparticles. Results showed a suitable mean size for oral administration (<600 nm by dynamic laser scattering), spherical shape, encapsulation efficiency (59.8%), and high recovery yield (80.6%). Circular dichroism spectroscopy demonstrated that protein retained its secondary structure after encapsulation. Moreover, the mucoadhesive potential of the nanoparticles was assessed in silico and the results, corroborated with ex-vivo experiments, showed that using chitosan strongly increases mucoadhesion. Besides, in vitro and in vivo safety assessment of the final formulation were performed, showing no toxicity. Lastly, the insulin-loaded nanoparticles were effective in reducing diabetic rats’ glycemia. Overall, the coating of insulin-loaded nanoparticles with chitosan represents a potentially safe and promising approach to protect insulin and enhance peroral delivery.

Viability of Porcine Corneal Epithelium Ex Vivo and Effect of Exposure to Air

Cornea ◽  
2004 ◽  
Vol 23 (7) ◽  
pp. 715-719 ◽  
Author(s):  
Emily Pik Yin Choy ◽  
Tony Shing Shun To ◽  
Pauline Cho ◽  
Iris Frances Forster Benzie ◽  
Camus Kar Man Choy
Keyword(s):  
Corneal Epithelium ◽  
Ex Vivo

scholarly journals Ex vivo models of human ocular surface regeneration indicate that conjunctiva possess the capacity of restoring corneal epithelium

2021 ◽  
Vol 99 (S265) ◽  
Author(s):  
Chantal Perrache ◽  
Sylvain Poinard ◽  
Philippe Gain ◽  
Gilles Thuret ◽  
Zhiguo He
Keyword(s):  
Corneal Epithelium ◽  
Ocular Surface ◽  
Ex Vivo ◽  
Surface Regeneration

scholarly journals Evaluating the Controlled Release Properties of Inhaled Nanoparticles Using Isolated, Perfused, and Ventilated Lung Models

2011 ◽  
Vol 2011 ◽  
pp. 1-16 ◽  
Author(s):  
Moritz Beck-Broichsitter ◽  
Thomas Schmehl ◽  
Werner Seeger ◽  
Tobias Gessler
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ex Vivo ◽  
Polymeric Nanoparticles ◽  
Polymeric Materials ◽  
Delivery Systems ◽  
Inhalation Therapy ◽  
Great Promise ◽  
Distribution Data ◽  
Isolated Lung

Polymeric nanoparticles meet the increasing interest for inhalation therapy and hold great promise to improve controlled drug delivery to the lung. The synthesis of tailored polymeric materials and the improvement of nanoparticle preparation techniques facilitate new perspectives for the treatment of severe pulmonary diseases. The physicochemical properties of such drug delivery systems can be investigated using conventional analytical procedures. However, the assessment of the controlled drug release properties of polymeric nanoparticles in the lung remains a considerable challenge. In this context, the isolated lung technique is a promising tool to evaluate the drug release characteristics of nanoparticles intended for pulmonary application. It allows measurements of lung-specific effects on the drug-release properties of pulmonary delivery systems.Ex vivomodels are thought to overcome the common obstacles ofin vitrotests and offer more reliable drug release and distribution data that are closer to thein vivosituation.

Formulation of polymeric nanoparticles of antidepressant drug for intranasal delivery

2019 ◽  
Vol 10 (11) ◽  
pp. 683-696 ◽  
Author(s):  
Parva Jani ◽  
Jigar Vanza ◽  
Nilima Pandya ◽  
Hemal Tandel
Keyword(s):  
Glycolic Acid ◽  
Ex Vivo ◽  
Polymeric Nanoparticles ◽  
Antidepressant Drug ◽  
Antidepressant Activity ◽  
Poloxamer 407 ◽  
Brain Drug Delivery ◽  
Immobility Time ◽  
Nanoprecipitation Method ◽  
Nasal Toxicity

Aim: The manuscript describes the performance of nanoparticles loaded with antidepressant drug for nose-to-brain drug delivery. Materials & methods: Poly-lactic-co-glycolic acid-loaded nanoparticles of agomelatine were prepared by nanoprecipitation method using poloxamer 407 as stabilizer. The process parameters were optimized using factorial design. Results: The drug-loaded nanoparticles having low particle size (<200 nm) with narrow size distribution and required zeta potential (-22.7 mV) to avoid aggregation showed sustained release profile and were found to have higher permeability as observed from ex vivo studies when compared with plain drug suspension. Histopathology test showed that the optimized formulation was free from nasal toxicity on the goat nasal mucosa. Pharmacodynamic study showed significant reduction in immobility time in rats treated with the formulation which indicated antidepressant activity of the formulation. Conclusion: The prepared agomelatin-loaded poly-lactic-co-glycolic acid nanoparticles showed prominent antidepressant activity by nose-to-brain delivery as observed from various studies.

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