scholarly journals Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 533
Author(s):  
Eloy Pena-Rodríguez ◽  
Maria Lajarin-Reinares ◽  
Aida Mata-Ventosa ◽  
Sandra Pérez-Torras ◽  
Francisco Fernández-Campos
Keyword(s):  
In Vitro Release ◽  
Human Keratinocytes ◽  
Topical Administration ◽  
In Vitro Cytotoxicity ◽  
Hair Follicles ◽  
Vertical Diffusion ◽  
Biodistribution Studies ◽  
Follicular Targeting ◽  
Depot Effect

Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated.

scholarly journals Preparation and Evaluation of Collagen-Based Patches as Curcumin Carriers

Polymers ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 2393
Author(s):  
Zoi Terzopoulou ◽  
Anna Michopoulou ◽  
Artemis Palamidi ◽  
Elena Koliakou ◽  
Dimitrios Bikiaris
Keyword(s):  
Topical Treatment ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Human Keratinocytes ◽  
Inhibitory Effect ◽  
Psoriatic Skin ◽  
Burst Release ◽  
Swelling Ratio ◽  
Natural Polyphenol

Patients with psoriasis are dissatisfied with the standard pharmacological treatments, whether systemic or topical, with many of them showing interest in complementary and alternative medicine. Curcumin (Cur), a natural polyphenol derived from turmeric, has recently gained attention for skin-related diseases because of its proven anti-inflammatory action. However, topical treatment with Cur would be inadequate because of its hydrophobicity, instability, and low bioavailability. In addition, hyperkeratosis and lack of moisture in psoriatic skin result in low penetration that would prevent actives from permeating the stratum corneum. In this work, a polymer-based formulation of Cur for the topical treatment of psoriasis is reported. To improve the physicochemical stability of Cur, it was first encapsulated in chitosan nanoparticles. The Cur-loaded nanoparticles were incorporated in a hydrophilic, biocompatible collagen-based patch. The nanoparticle-containing porous collagen patches were then chemically cross-linked. Morphology, chemical interactions, swelling ratio, enzymatic hydrolysis, and Cur release from the patches were evaluated. All patches showed excellent swelling ratio, up to ~1500%, and after cross-linking, the pore size decreased, and their hydrolysis rates decelerated. The in vitro release of Cur was sustained with an initial burst release, reaching 55% after 24 h. Cur within the scaffolds imparted a proliferation inhibitory effect on psoriatic human keratinocytes in vitro.

scholarly journals Incorporation of a Hydrophilic Spacer Reduces Hepatic Uptake of HER2-Targeting Affibody–DM1 Drug Conjugates

Cancers ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 1168
Author(s):  
Haozhong Ding ◽  
Mohamed Altai ◽  
Sara S. Rinne ◽  
Anzhelika Vorobyeva ◽  
Vladimir Tolmachev ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Histopathological Examination ◽  
Specific Binding ◽  
Hepatic Uptake ◽  
In Vitro Cytotoxicity ◽  
Drug Conjugates ◽  
Biodistribution Studies ◽  
Development Approach

Affibody molecules are small affinity-engineered scaffold proteins which can be engineered to bind to desired targets. The therapeutic potential of using an affibody molecule targeting HER2, fused to an albumin-binding domain (ABD) and conjugated with the cytotoxic maytansine derivate MC-DM1 (AffiDC), has been validated. Biodistribution studies in mice revealed an elevated hepatic uptake of the AffiDC, but histopathological examination of livers showed no major signs of toxicity. However, previous clinical experience with antibody drug conjugates have revealed a moderate- to high-grade hepatotoxicity in treated patients, which merits efforts to also minimize hepatic uptake of the AffiDCs. In this study, the aim was to reduce the hepatic uptake of AffiDCs and optimize their in vivo targeting properties. We have investigated if incorporation of hydrophilic glutamate-based spacers adjacent to MC-DM1 in the AffiDC, (ZHER2:2891)2–ABD–MC-DM1, would counteract the hydrophobic nature of MC-DM1 and, hence, reduce hepatic uptake. Two new AffiDCs including either a triglutamate–spacer–, (ZHER2:2891)2–ABD–E3–MC-DM1, or a hexaglutamate–spacer–, (ZHER2:2891)2–ABD–E6–MC-DM1 next to the site of MC-DM1 conjugation were designed. We radiolabeled the hydrophilized AffiDCs and compared them, both in vitro and in vivo, with the previously investigated (ZHER2:2891)2–ABD–MC-DM1 drug conjugate containing no glutamate spacer. All three AffiDCs demonstrated specific binding to HER2 and comparable in vitro cytotoxicity. A comparative biodistribution study of the three radiolabeled AffiDCs showed that the addition of glutamates reduced drug accumulation in the liver while preserving the tumor uptake. These results confirmed the relation between DM1 hydrophobicity and liver accumulation. We believe that the drug development approach described here may also be useful for other affinity protein-based drug conjugates to further improve their in vivo properties and facilitate their clinical translatability.

In Vitro Release: Comparative Evaluation of Vertical Diffusion Cell System and Automated Procedure

2003 ◽  
Vol 8 (1) ◽  
pp. 97-102 ◽  
Author(s):  
Vinod P. Shah ◽  
Jerome Elkins ◽  
Steve Shaw ◽  
Royal Hanson
Keyword(s):  
Comparative Evaluation ◽  
In Vitro Release ◽  
Cell System ◽  
Diffusion Cell ◽  
Vertical Diffusion ◽  
Vitro Release

In vitro cytotoxicity of CdSe/ZnS quantum dots with different surface coatings to human keratinocytes HaCaT cells

2013 ◽  
Vol 25 (1) ◽  
pp. 163-171 ◽  
Author(s):  
Kavitha Pathakoti ◽  
Huey-Min Hwang ◽  
Hong Xu ◽  
Zoraida P. Aguilar ◽  
Andrew Wang
Keyword(s):  
Quantum Dots ◽  
Human Keratinocytes ◽  
In Vitro Cytotoxicity ◽  
Surface Coatings ◽  
Hacat Cells

scholarly journals Development of a Topical Amphotericin B and Bursera graveolens Essential Oil-Loaded Gel for the Treatment of Dermal Candidiasis

2021 ◽  
Vol 14 (10) ◽  
pp. 1033
Author(s):  
Lupe Carolina Espinoza ◽  
Lilian Sosa ◽  
Paulo C. Granda ◽  
Nuria Bozal ◽  
Natalia Díaz-Garrido ◽  
...  
Keyword(s):  
Essential Oil ◽  
Amphotericin B ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Topical Administration ◽  
In Vivo Models ◽  
Topical Gel ◽  
Cutaneous Candidiasis ◽  
Vitro Release

The higher molecular weight and low solubility of amphotericin B (AmB) hinders its topical administration. The aim of this study was to incorporate Bursera graveolens essential oil into an AmB topical gel (AmB + BGEO gel) in order to promote the diffusion of the drug through the skin in the treatment of cutaneous candidiasis. AmB + BGEO gel formulation was determined using a factorial experiment. Physical and chemical parameters, stability, in vitro release profile and ex vivo permeation in human skin were evaluated. In vitro antimicrobial activity was studied using strains of C. albicans, C. glabrata and C. parapsilosis. The tolerability was evaluated using in vitro and in vivo models. AmB + BGEO gel presented appropriate characteristics for topical administration, including pH of 5.85, pseudoplastic behavior, optimal extensibility, as well as high stability and acceptable tolerability. In vitro release studies showed that the formulation releases the drug following a Boltzmann sigmoidal model. Finally, AmB + BGEO gel exhibited higher amount of drug retained inside the skin and lower Minimum Inhibitory Concentration than a formulation sans essential oil. Therefore, these results suggest that the incorporation of B. graveolens essential oil in the formulation could be used as strategy to promote a local effect in the treatment of cutaneous candidiasis.

scholarly journals In Vitro Release Testing Methodology and Variability with the Vertical Diffusion Cell (VDC)

2018 ◽  
Vol 25 (3) ◽  
pp. 52-61 ◽  
Author(s):  
Ryan R Klein ◽  
Jenna L Heckart ◽  
Kailas D Thakker
Keyword(s):  
In Vitro Release ◽  
Diffusion Cell ◽  
Vertical Diffusion ◽  
Testing Methodology ◽  
Vitro Release ◽  
Release Testing

scholarly journals Nanocellulose-Based Patches Loaded with Hyaluronic Acid and Diclofenac towards Aphthous Stomatitis Treatment

Nanomaterials ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 628 ◽  
Author(s):  
João P. F. Carvalho ◽  
Ana C. Q. Silva ◽  
Verónica Bastos ◽  
Helena Oliveira ◽  
Ricardo J. B. Pinto ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
In Vitro Release ◽  
Three Dimensional ◽  
Human Keratinocytes ◽  
Controlled Drug Release ◽  
Dynamic Mechanical Properties ◽  
Aphthous Stomatitis ◽  
Release Mechanism ◽  
Porous Network

Nanostructured patches composed of bacterial nanocellulose (BNC), hyaluronic acid (HA) and diclofenac (DCF) were developed, envisioning the treatment of aphthous stomatitis. Freestanding patches were prepared via diffusion of aqueous solutions of HA and DCF, with different concentrations of DCF, into the wet BNC three-dimensional porous network. The resultant dual polysaccharides-based patches with a nanostructured morphology present thermal stability up to 200 °C, as well as good dynamic mechanical properties, with a storage modulus higher than 1.0 GPa. In addition, the patches are non-cytotoxic to human keratinocytes (HaCaT cells), with a cell viability of almost 100% after 24 h. The in vitro release profile of DCF from the patches was evaluated in simulated saliva, and the data refer to a diffusion- and swelling-controlled drug-release mechanism. The attained results hint at the possibility of using these dual polysaccharides-based oral mucosal patches to target aphthous stomatitis.

scholarly journals Assessment of “Sameness” and/or Differences between Marketed Creams Containing Miconazole Nitrate Using a Discriminatory in vitro Release Testing (IVRT) Method

2020 ◽  
Vol 88 (1) ◽  
pp. 6
Author(s):  
Potiwa Purazi ◽  
Seeprarani Rath ◽  
Ashmita Ramanah ◽  
Isadore Kanfer
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Vertical Diffusion ◽  
Discriminatory Ability ◽  
Miconazole Nitrate ◽  
Performance Verification Test ◽  
Semi Solid ◽  
Vitro Release ◽  
Release Testing

In vitro release testing (IVRT) provides an efficient method for the evaluation of drug release from semi-solid formulations. The aim of this research was to develop and validate a discriminatory IVRT system using vertical diffusion cells (VDCs) to assess generic topical products containing miconazole nitrate (MCZ). A comprehensive approach addressing all essential suitability criteria supporting the reliability of IVRT results was applied. These include mechanical validation of the VDCs, a performance verification test (PVT), validation of the analytical method (HPLC) used to quantify the drug release and validation of the IVRT method to confirm its precision, reproducibility, discriminatory ability, and robustness. Two marketed generic products were tested and assessed in accordance with the acceptance criteria for “sameness” in the FDA’s SUPAC-SS guidance which requires that the 90% confidence interval (CI) should fall within the limits of 75%–133.33%. One product was found to be in vitro equivalent to the reference product whereas the other was not. The results confirmed the suitability of the IVRT method to accurately measure the release of MCZ from topical cream products and, importantly, demonstrated the necessary discriminatory ability to assess “sameness”/differences of dermatological creams containing MCZ. Furthermore, the developed IVRT method was able to detect differences between formulations, which may be attributed to qualitative (Q1) and quantitative (Q2) properties and the microstructure and arrangement of matter (Q3).

Analysis of Process and Formulation Variables on Chitosan based Losartan Potassium Nanoparticles: Preparation, Validation and in vitro Release Kinetics

2020 ◽  
Vol 13 (1) ◽  
pp. 41-54
Author(s):  
Manisha Singh ◽  
Ramneek Kaur ◽  
Rashi Rajput ◽  
Shriya Agarwal ◽  
Sachin Kumar ◽  
...  
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
In Vitro Cytotoxicity ◽  
Model Systems ◽  
Oral Dosage ◽  
Losartan Potassium ◽  
Size Analysis ◽  
Angiotensin Ii Receptor ◽  
Tem Analysis

Background: Although many potential therapeutic compounds have been discovered and have exhibited a promising recovery, their effective delivery in the human system has always remained questionable with many pharmacological constraints in delivering them. Amidst all this, the concept of nanomedicine has always assured the potential to overcome the drug delivery complications in the present treatment methods. Losartan Potassium (LP) is indicated in the management of hypertension. Owing to its moderate bioavailability (32%) and a number of side effects due to the oral dosage forms of LP thus, nanoparticles based delivery would be beneficial. Objective: The present study is focused to develop a nanoparticle system of Losartan Potassium, an Angiotensin II receptor antagonist and a well-known promising antihypertensive drug, to conquer its limitation of bioavailability and potential adverse effects. Method: LP Loaded Polymeric Nanoparticles (LP-NPs) were developed by ionic gelation method using Chitosan (CH) and Tripolyphosphate (TPP) for cross linkage in various optimising ratios. After the successful optimisation and synthesis of LP-NPs, the optimised formulation was further characterized by Particle Size Analysis (PSA), Polydispersity Index (PDI), Zeta Potential (ZP), TEM analysis with the in vitro cytotoxicity and permeability evaluation. Results: The results showed the average size of 123.5 ± 1.23nm with polydispersibility score of 0.257 ± 0.079 and charge of -2.74 mV respectively. Further, Transmission Electron Microscopy (TEM) images showed the size range in almost conformity with DLS findings, representing the spherical and smooth morphology. In vitro drug release kinetics estimation showed sustained release routine of the drug and the cell viability studies done on Jurkat cell line displayed lesser cytotoxicity of LP-NPs (99.3 ± 2.28% and 98.17 ± 1.86%) in comparison with the LP only (85.3 ± 2.1% and 71.7 ± 1.07%) at different time periods (12 hours and 24 hours). Conclusion: The aforementioned results confirm the effective fabrication of LP-NPs and indicate that it may further, used on higher model systems to investigate the above parameters and their enhanced effectiveness in hypertension.

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