scholarly journals Development and Evaluation of Azelaic Acid-Loaded Microemulsion for Transfollicular Drug Delivery Through Guinea Pig Skin: A Mechanistic Study

2020 ◽  
Vol 10 (2) ◽  
pp. 239-246 ◽  
Author(s):  
Anayatollah Salimi ◽  
Behzad Sharif Makhmal Zadeh ◽  
Salar Godazgari ◽  
Abbas Rahdar
Keyword(s):  
Diffusion Coefficient ◽  
Guinea Pig ◽  
Azelaic Acid ◽  
Drug Carrier ◽  
Mechanistic Study ◽  
Skin Permeability ◽  
Antibacterial Drug ◽  
Drug Release Profile ◽  
Hairy Skin ◽  
Drug Flux

Purpose: Azelaic acid is a natural keratolytic, comedolytic, and antibacterial drug that is used to treat acne. The topical application of azelaic acid is associated with problems such as irritation and low permeability. For dissolving, the problem is that microemulsion (ME) is used as a drug carrier. The aim of this study was to increase the azelaic acid affinity in the follicular pathway through ME. Methods: Azelaic acid-loaded MEs were prepared by the water titration method. The properties of the MEs included formulation stability, particle size, drug release profile, thermal behavior of MEs, the diffusion coefficient of the MEs and skin permeability in the non-hairy ear skin and hairy abdominal skin of guinea pig were studied in situ. Results: The MEs demonstrated a mean droplet size between 5 to 150 nm. In the higher ratios of surfactant/co-surfactant, a more extensive ME zone was found. All MEs increased the azelaic acid flux through both hairy and non-hairy skin compared with an aqueous solution of azelaic acid as a control. This effect of the ME was mainly dependent on the droplet diffusion coefficient and hydrodynamic radius. MEs with a higher diffusion coefficient demonstrated higher azelaic acid flux through hairy and non-hairy skin. Drug flux through both skins was affected by the surfactant/co-surfactant ratio in that the higher ratio increased the azelaic acid affinity into the follicular pathway. Conclusion: Finally, the ME with the highest droplet diffusion coefficient and the lowest surfactant/co-surfactant ratio was the best ME for azelaic acid delivery into the follicular pathway.

Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Anti Cancer ◽  
Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

Evaluation of effectiveness of combined use of COC and topical preparation containing azelaic acid for acne

2021 ◽  
pp. 24-28
Author(s):  
L. S. Kruglova ◽  
N. V. Gryazeva
Keyword(s):  
Azelaic Acid ◽  
Comparable Efficacy ◽  
Antibacterial Drug ◽  
Global Assessment Scale ◽  
Efficiency Assessment ◽  
Combined Use ◽  
Comparison Groups ◽  
Group 2 ◽  
Group 1

The article presents the results of evaluating the effectiveness of the combined use of combined oral contraceptives (COC) and Skinoren cream in severe papular-pustular and moderate nodular-cystic acne.Material and methods. Patients of the first group (n = 11) used COC and an external antibacterial drug two times a day for the treatment of acne. Patients of the second group (n = 12) used COC and an external drug containing azelaic acid (Skinoren) for the treatment of acne two times a day. The duration of follow-up was 6 months. The efficiency assessment was carried out taking into account the dynamics of the indicators of the IGA (Investors Global Assessment) scale. The Manchester Scar Scale (MSS) was used to assess the effectiveness of post-acne correction. In addition, the effectiveness was evaluated based on the results of the mexametry.Results. When evaluating IGA in the comparison groups in patients with severe papulopustular acne and moderate nodular cystic acne, comparable efficacy was noted, but the best results were recorded in the COC + Skinoren group (p < 0.05). No effect and deterioration of the condition were observed in any group. When assessing MSS, the most pronounced changes were observed in patients of group 2, where the combination of COC + Skinoren was used. So, in group 1, the severity of scars decreased by 42.3 %, in group 2 by 48.2 % (p < 0.05). The evaluation of the results of the mexametry showed a more pronounced decrease in the amount of pigment in patients from group 2. When studying the results of the severity of erythema, the dynamics similar to the severity of the pigment was obtained. The best result was registered in group 2 (COC + Skinoren) (p < 0.05).Conclusions. The combined use of COC and Skinoren cream for severe papular-pustular and moderate nodular-cystic acne has proven to be an effective method both in relation to the number of inflammatory and retention elements, and in relation to hyperpigmentation.

Biopolymer Encapsulation of CdTe Quantum Dot for In Vitro Controlled Drug Delivery Release of 6-Mercaptopurine

2012 ◽  
Vol 584 ◽  
pp. 258-262 ◽  
Author(s):  
Sundarrajan Parani ◽  
Baddireddi Subhadra Lakshmi ◽  
Kanniyan Pandian
Keyword(s):  
Drug Delivery ◽  
Folic Acid ◽  
Quantum Dot ◽  
Drug Carrier ◽  
Controlled Drug Delivery ◽  
Release Profile ◽  
Drug Release Profile ◽  
The Stability ◽  
Cdte Quantum Dot

Alginate biopolymer stabilized CdTe quantum dot (QD) was prepared and it was encapsulated with folic acid conjugated chitosan for controlled drug delivery of anticancer drug 6-mercaptopurine (6-MP). In addition to alginate, chitosan enhances the stability of QD. Also, in addition to chitosan, alginate binds to the drug leading to enhance the loading efficiency of the resulting drug carrier. The drug release profile of the carrier was investigated by in-vitro. The present study has shown that this drug carrier is feasible for drug delivery and will be important beneficiary for cancer therapy.

Nanocomposite Multilayer Fibrous Membrane for Sustained Drug Release

2014 ◽  
Vol 894 ◽  
pp. 364-368 ◽  
Author(s):  
Ahmed Hassanin ◽  
Ahmed A. El-Moneim ◽  
Mohamed Ghaniem ◽  
Hassan Nageh
Keyword(s):  
Drug Release ◽  
Outer Layer ◽  
Biomedical Application ◽  
Drug Carrier ◽  
Electrospun Nanofibers ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Sem Images ◽  
Fibrous Membranes ◽  
The Many

Building on the success of the many earlier studies on electrospun nanofibers technique which provide a non woven web to the order of nanometers introducing superior properties such as large surface area, superior mechanical properties and ease of implementation in many fields of applications, elctrospun nanofibers became an important issue for many researchers in various fields. Using elctrospun fibers as a drug carrier, is showing a huge promising potential for the future of biomedical application. Our work in this research is focusing on engineering a system to control the drug release profile rate especially for wound dressing. Nanocomposite multilayer fibrous membranes, using electrospinning method, have been developed for drug release in form of sandwich structure of three layers. Inner layer which is kept Polycaprolactane (PCL) loaded with drug. The two outer layers have been changed with different blend ratios between Chitosan (Cs) and PCL as follow [0%:100% Cs:PCL, 30%:70% Cs:PCL, 50%:50% Cs:PCL, 70%:30% Cs:PCL]. The results showed that the release rate has been affected dramatically by the outer layer composition. SEM images showed changing in the morphology due to the different in the composition of outer layer.

scholarly journals Hydroxyapatite/nifuroxazide conjugate: Characterization, drug release and antimicrobial activity

2021 ◽  
pp. 40-40
Author(s):  
Zeljko Radovanovic ◽  
Katarina Mihajlovski ◽  
Lidija Radovanovic ◽  
Djordje Janackovic ◽  
Rada Petrovic
Keyword(s):  
Drug Release ◽  
Raw Materials ◽  
Drug Carrier ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Antibacterial Drug ◽  
Stomach Acid ◽  
Poorly Soluble ◽  
Good Biocompatibility

Synthetic hydroxyapatite (Ca10(PO4)6(OH)2, HAp) is very similar to the inorganic part of the bones and teeth of mammals. It is a well-known biomaterial with good biocompatibility, osteoconductivity and bioactivity. Nifuroxazide (C12H9N3O5, NFX) is a broad-spectrum antibacterial drug and poorly soluble in water. In order to increase the solubility of NFX, nanosized HAp powder and raw NFX drug were mixed giving, as a result, HAp/NFX conjugate. Characterization of the raw materials and the obtained conjugate confirmed the integration of NFX on the HAp surface. The in vitro study of drug release in simulated stomach acid and intestinal fluid showed a much faster release of NFX from HAp surface than those of raw drug. HAp/NFX conjugate showed an excellent inhibitory effect against Gram-positive bacterium Staphylococcus aureus, Gram-negative bacterium Escherichia coli and yeast Candida albicans, proving the nanosized HAp powder as a promising drug carrier.

scholarly journals 3D Bioprinting of the Sustained Drug Release Wound Dressing with Double-Crosslinked Hyaluronic-Acid-Based Hydrogels

Polymers ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 1584 ◽  
Author(s):  
Si ◽  
Xing ◽  
Ding ◽  
Zhang ◽  
Yin ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Drug Release ◽  
Wound Dressing ◽  
Wound Repair ◽  
Click Reaction ◽  
Antibacterial Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Rheological Test

：Hyaluronic acid (HA)-based hydrogels are widely used in biomedical applications due to their excellent biocompatibility. HA can be Ultraviolet (UV)-crosslinked by modification with methacrylic anhydride (HA-MA) and crosslinked by modification with 3,3'-dithiobis(propionylhydrazide) (DTP) (HA-SH) via click reaction. In the study presented in this paper, a 3D-bioprinted, double-crosslinked, hyaluronic-acid-based hydrogel for wound dressing was proposed. The hydrogel was produced by mixing HA-MA and HA-SH at different weight ratios. The rheological test showed that the storage modulus (G') of the HA-SH/HA-MA hydrogel increased with the increase in the HA-MA content. The hydrogel had a high swelling ratio and a high controlled degradation rate. The in vitro degradation test showed that the hydrogel at the HA-SH/HA-MA ratio of 9:1 (S9M1) degraded by 89.91% ± 2.26% at 11 days. The rheological performance, drug release profile and the cytocompatibility of HA-SH/HA-MA hydrogels with loaded Nafcillin, which is an antibacterial drug, were evaluated. The wound dressing function of this hydrogel was evaluated by Live/Dead staining and CCK-8 assays. The foregoing results imply that the proposed HA-SH/HA-MA hydrogel has promise in wound repair applications.

scholarly journals Effects of the Fluoroquinolone Antibacterial Drug Ciprofloxacin on Ventricular Repolarization in the Halothane-Anesthetized Guinea Pig

2013 ◽  
Vol 122 (3) ◽  
pp. 205-212 ◽  
Author(s):  
Kazuhiro Matsuo ◽  
Kaori Fujiwara ◽  
Naoki Omuro ◽  
Itsuki Kimura ◽  
Kazuko Kobayashi ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Ventricular Repolarization ◽  
Antibacterial Drug

scholarly journals Development of a Model Based on Physical Mechanisms for the Explanation of Drug Release: Application to Diclofenac Release from Polyurethane Films

Polymers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1230
Author(s):  
Navideh Abbasnezhad ◽  
Mohamed Kebdani ◽  
Mohammadali Shirinbayan ◽  
Stéphane Champmartin ◽  
Abbas Tcharkhtchi ◽  
...  
Keyword(s):  
Experimental Data ◽  
Drug Release ◽  
Water Solution ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Linear Optimization ◽  
Programming Algorithm ◽  
Burst Release ◽  
Drug Release Profile ◽  
Physical Mechanisms

In this study, we present a method for prediction of the drug-release profile based on the physical mechanisms that can intervene in drug release from a drug-carrier. The application presented here incorporates the effects of drug concentration and Reynolds number defining the circulating flow in the testing vein. The experimental data used relate to the release of diclofenac from samples of non-degradable polyurethane subjected to static and continuous flow. This case includes simultaneously three mechanisms: burst-release, diffusion and osmotic pressure, identified beforehand here as being able to contribute to the drug liberation. For this purpose, authors coded the Sequential Quadratic Programming Algorithm to solve the problem of non-linear optimization. The experimental data used to develop the mathematical model obtained from release studies carried out in water solution at 37 °C, for three concentrations of diclofenac and two water flow rates. We discuss the contribution of mechanisms and kinetics by considering two aforementioned parameters and, following that, we obtain the specific-model and compare the calculated results with the experimental results for the reserved cases. The results showed that drug percentage mostly affect the burst release, however flow rate has affected the osmotic release. In addition, release kinetics of all the mechanisms have increased by increasing the values of two considered parameters.

scholarly journals Noncytotoxic polycaprolactone-polyethyleneglycol-ε-poly(l-lysine) triblock copolymer synthesized and self-assembled as an antibacterial drug carrier

RSC Advances ◽  
2017 ◽  
Vol 7 (63) ◽  
pp. 39718-39725 ◽  
Author(s):  
Chuncai Zhou ◽  
Xinyu Zhou ◽  
Xiaokai Su
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Triblock Copolymer ◽  
Drug Carrier ◽  
Antibacterial Drug ◽  
Self Assembled ◽  
Low Cytotoxicity

The PCL35-b-PEG45-b-EPL23 vesicles perform well in vitro drug release and antibacterial activity against Gram− and Gram+ bacteria with low cytotoxicity.

Sign in / Sign up

Export Citation Format

Share Document