scholarly journals Niosome encapsulated doxycycline-hyclate for potentiation of acne therapy: formulation and characterization

2021 ◽  
Author(s):  
fatemeh kashani asadi jafari ◽  
afra Hadjizadeh
Keyword(s):  
Antibacterial Activity ◽  
Entrapment Efficiency ◽  
Fold Increase ◽  
Wistar Rat ◽  
Dermal Fibroblasts ◽  
Rat Skin ◽  
Doxycycline Hyclate ◽  
Drug Deposition ◽  
Wide Range

Acne is the pilosebaceous units' disorder. The most important cause of acne is the colonization of bacteria in the follicles. Among antibiotics, doxycycline-hyclate kills a wide range of bacteria. To prevent oral administration's side effects, overcome the barriers of conventional topical treatment, and improve the therapeutic effectiveness, doxycycline-hyclate was loaded into four niosomal formulations with different percentages of constituents (span 60 and cholesterol) prepared by the thin-film hydration method. Then, one of the four formulations with the most appropriate particle size of 362.88 ± 13.05 nm to target the follicles, percentage of drug entrapment efficiency of 56.3 ± 2.1%, in vitro drug release of 54.93 ± 1.99% after 32 hours, and the lowest permeation of the drug through the Wistar rat skin, was selected. Then, its toxicity on human dermal fibroblasts (HDF) by MTT method after 72 hours, its antibacterial activity against the main acne-causing bacteria via antibiogram test, and its effect on Wistar rat skin drug deposition were measured. Improved cell viability, increased antibacterial activity, and an approximately three-fold increase in drug deposition were the optimal niosomal formulation features relative to the free drug. Overall, this study demonstrated the ability of nano-niosomes containing doxycycline-hyclate to treat skin acne.

scholarly journals Mutual influence of selenium nanoparticles and FGF2-STAB® on biocompatible properties of collagen/chitosan 3D scaffolds: in vitro and ex ovo evaluation

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Johana Muchová ◽  
Vanessa Hearnden ◽  
Lenka Michlovská ◽  
Lucie Vištejnová ◽  
Anna Zavaďáková ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Metabolic Activity ◽  
Mutual Influence ◽  
Chorioallantoic Membrane ◽  
Antagonistic Effect ◽  
Dermal Fibroblasts ◽  
Selenium Nanoparticles ◽  
Freeze Dried ◽  
Chitosan Scaffolds

AbstractIn a biological system, nanoparticles (NPs) may interact with biomolecules. Specifically, the adsorption of proteins on the nanoparticle surface may influence both the nanoparticles' and proteins' overall bio-reactivity. Nevertheless, our knowledge of the biocompatibility and risk of exposure to nanomaterials is limited. Here, in vitro and ex ovo biocompatibility of naturally based crosslinked freeze-dried 3D porous collagen/chitosan scaffolds, modified with thermostable fibroblast growth factor 2 (FGF2-STAB®), to enhance healing and selenium nanoparticles (SeNPs) to provide antibacterial activity, were evaluated. Biocompatibility and cytotoxicity were tested in vitro using normal human dermal fibroblasts (NHDF) with scaffolds and SeNPs and FGF2-STAB® solutions. Metabolic activity assays indicated an antagonistic effect of SeNPs and FGF2-STAB® at high concentrations of SeNPs. The half-maximal inhibitory concentration (IC50) of SeNPs for NHDF was 18.9 µg/ml and IC80 was 5.6 µg/ml. The angiogenic properties of the scaffolds were monitored ex ovo using a chick chorioallantoic membrane (CAM) assay and the cytotoxicity of SeNPs over IC80 value was confirmed. Furthermore, the positive effect of FGF2-STAB® at very low concentrations (0.01 µg/ml) on NHDF metabolic activity was observed. Based on detailed in vitro testing, the optimal concentrations of additives in the scaffolds were determined, specifically 1 µg/ml of FGF2-STAB® and 1 µg/ml of SeNPs. The scaffolds were further subjected to antimicrobial tests, where an increase in selenium concentration in the collagen/chitosan scaffolds increased the antibacterial activity. This work highlights the antimicrobial ability and biocompatibility of newly developed crosslinked collagen/chitosan scaffolds involving FGF2-STAB® and SeNPs. Moreover, we suggest that these sponges could be used as scaffolds for growing cells in systems with low mechanical loading in tissue engineering, especially in dermis replacement, where neovascularization is a crucial parameter for successful skin regeneration. Due to their antimicrobial properties, these scaffolds are also highly promising for tissue replacement requiring the prevention of infection.

scholarly journals Exosome-Mediated Insulin Delivery for the Potential Treatment of Diabetes Mellitus

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1870
Author(s):  
Belén Rodríguez-Morales ◽  
Marilena Antunes-Ricardo ◽  
José González-Valdez
Keyword(s):  
Diabetes Mellitus ◽  
Human Insulin ◽  
Insulin Delivery ◽  
Dermal Fibroblasts ◽  
Therapeutic Drug ◽  
Extracellular Medium ◽  
Glucose Levels ◽  
Wide Range ◽  
Diabetes Mellitus Treatment

Exosomes are extracellular nanovesicles between 30 and 150 nm that serve as essential messengers for different biological signaling and pathological processes. After their discovery, a wide range of applications have been developed, especially in therapeutic drug delivery. In this context, the aim of this work was to test the efficiency of exosome-mediated human insulin delivery using exosomes extracted from three different cell lines: hepatocellular carcinoma (HepG2); primary dermal fibroblasts (HDFa) and pancreatic β cells (RIN-m); all are related to the production and/or the ability to sense insulin and to consequently regulate glucose levels in the extracellular medium. The obtained results revealed that the optimal insulin loading efficiency was achieved by a 200 V electroporation, in comparison with incubation at room temperature. Moreover, the maximum in vitro exosome uptake was reached after incubation for 6 h, which slightly decreased 24 h after adding the exosomes. Glucose quantification assays revealed that exosome-mediated incorporation of insulin presented significant differences in HDFa and HepG2 cells, enhancing the transport in HDFa, in comparison with free human insulin effects in the regulation of extracellular glucose levels. No significant differences were found between the treatments in RIN-m cells. Hence, the results suggest that exosomes could potentially become a valuable tool for stable and biocompatible insulin delivery in diabetes mellitus treatment alternatives.

scholarly journals P11.39 Chloroquine as an anti-glioblastoma therapeutic: repurposing of an old drug

2019 ◽  
Vol 21 (Supplement_3) ◽  
pp. iii51-iii52
Author(s):  
L Roy ◽  
M Poirier ◽  
D Fortin
Keyword(s):  
Median Survival ◽  
Transforming Growth Factor Beta ◽  
Transforming Growth Factor ◽  
Plasma Concentrations ◽  
Progression Free Survival ◽  
Fold Increase ◽  
Wistar Rat ◽  
Control Group ◽  
Primary Brain Tumour

Abstract BACKGROUND Glioblastoma (GBM) is the most common and aggressive type of primary brain tumour in adults. These tumours depict anarchic proliferation and brain infiltration as well as radio- and chemoresistant profiles. The complete surgical resection is unachievable and responses to standard therapy are transitory. Recurrence is thus inevitable and patient prognosis is generally less than 15 months. Transforming growth factor-beta (TGF-β) holds a substantial role in supporting the GBM phenotype. We showed that TGF-β 1 expression levels correlate with overall and progression-free survival in newly diagnosed GBM patient. We also observed that chloroquine (CQ) can reduce the production of TGF-β together with proliferation, invasion, radioresistance and radio-induced invasion in vitro. Unfortunately, little is known regarding the ability of CQ to penetrate the blood-brain barrier (BBB). Therefore, our objective is to determine whether intravenous (IV) or intra-arterial (IA) infusions of CQ and hydroxychloroquine (HCQ), a pharmacological analog of CQ, can yield therapeutic brain concentrations. MATERIAL AND METHODS To assess BBB penetration, the brain, plasma and cerebrospinal fluid (CSF) concentrations of CQ/HCQ were measured by LCMS/MS at different timepoints post-IV or post-IA infusions with 20 mg/kg of CQ/HCQ in tumour-free Wistar rat. For the survival studies, We implanted 10’000 F98 murin glioblastoma cells in the right putamen of Fischer rats. Ten days post-implantation, IA and IV infusion were accomplished through cannulations of the external right carotid and tail vein respectively. RESULTS With IV injections, CQ/HCQ brain concentrations 15 minutes post-injection reached 15.76 mg/g (0.18 µM) and 1.67 mg/g (0.078 µM) respectively. However, following IA infusions, we observed a 1.74 and 20.9 fold increase (20 mg/kg HCQ) as well as 7.1 and 84.7-fold-increase (20 mg/kg CQ) in contra- and ipsilateral brain concentrations respectively. Although brain concentrations gradually decreased over time post-IA infusions, the ipsilateral hemisphere CQ concentration was still 82.81 mg/g (34.52 µM) after 6 hours. Whereas plasma concentrations were very similar following IV and IA infusions, both molecules barely accumulated in the CSF and only when using IA infusions. The median survival of the control group (IA phosphate-buffered saline) and the group treated with 20 mg/kg CQ IV were 23.5 days and 24.5 days respectively. However, rats injected with 20 mg/kg CQ IA had a median survival of 28.5 days. CONCLUSION These results suggest that IA CQ could be used to abrogate the GBM phenotype. As TGF-β is associated with resistance to both radio- and chemotherapy, we plan to characterize the combination of IA infusions of CQ in combination with radiation or chemotherapy (carboplatin).

scholarly journals Boosting the Brain Delivery of Atazanavir through Nanostructured Lipid Carrier-Based Approach for Mitigating NeuroAIDS

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1059
Author(s):  
Saif Ahmad Khan ◽  
Saleha Rehman ◽  
Bushra Nabi ◽  
Ashif Iqubal ◽  
Nida Nehal ◽  
...  
Keyword(s):  
Targeted Delivery ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Fold Increase ◽  
Pharmacokinetic Studies ◽  
Nanostructured Lipid Carrier ◽  
Brain Delivery ◽  
The Brain

Atazanavir (ATZ) presents poor brain availability when administered orally, which poses a major hurdle in its use as an effective therapy for the management of NeuroAIDS. The utilization of nanostructured lipid carriers (NLCs) in conjunction with the premeditated use of excipients can be a potential approach for overcoming the limited ATZ brain delivery. Methods: ATZ-loaded NLC was formulated using the quality by design-enabled approach and further optimized by employing the Box–Behnken design. The optimized nanoformulation was then characterized for several in vitro and in vivo assessments. Results: The optimized NLC showed small particle size of 227.6 ± 5.4 nm, high entrapment efficiency (71.09% ± 5.84%) and high drug loading capacity (8.12% ± 2.7%). The release pattern was observed to be biphasic exhibiting fast release (60%) during the initial 2 h, then trailed by the sustained release. ATZ-NLC demonstrated a 2.36-fold increase in the cumulative drug permeated across the rat intestine as compared to suspension. Pharmacokinetic studies revealed 2.75-folds greater Cmax in the brain and 4-fold improvement in brain bioavailability signifying the superiority of NLC formulation over drug suspension. Conclusion: Thus, NLC could be a promising avenue for encapsulating hydrophobic drugs and delivering it to their target site. The results suggested that increase in bioavailability and brain-targeted delivery by NLC, in all plausibility, help in improving the therapeutic prospects of atazanavir.

Preparation, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Bovine Serum Album Nanoparticles

2011 ◽  
Vol 345 ◽  
pp. 349-354 ◽  
Author(s):  
Jia Lei Li ◽  
Yuan Gang Zu ◽  
Xiu Hua Zhao ◽  
Dong Mei Zhao ◽  
Xiao Qiang Chen ◽  
...  
Keyword(s):  
Bovine Serum ◽  
Biological Activities ◽  
Cardiovascular Effects ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Nano Technology ◽  
Beneficial Effects ◽  
Wide Range

Resveratrol (RES) is a naturally occurring triphenolic phytoalexin compound exerting numerous beneficial effects in the organism. It has a wide range of biological activities in vitro as well as in vivo, such as anti-cancer, antioxidant, anti-inflammatory and beneficial cardiovascular effects. But, its low solubility in water led to its poor absorption in vivo and low bioavailability. Bovine serum album (BSA) nanoparticles have emerged as versatile desired carrier systems due to its ready availability, biodegradability, lack of toxicity and immunogenicity with fast development of nano technology. In this study, RES-BSANPS were prepared by a desolvation method and chemical cross-linking with glutaraldehyde successfully. Results controlled conditions (concentration of BSA, 10 mg/ml; pH = 9.0; volume of ethanol, 6 ml; volume of 0.25 % glutaraldehyde, 100 µl; amount of RES, 6.7 mg; cross-linking time, 24 h at room temperature (1 ml/min)) for entrapment efficiency, loading efficiency, mean particle size and zeta potential, were found to be 88.7 %, 39.4 %, 175.4 ± 0.5 nm, -35.93 ± 0.79 mV, respectively.

scholarly journals Antibacterial Activity of Manuka Honey Against Azithromycin Resistant Extensively Drug Resistant Salmonella Typhi Clinical Isolates: In-Vitro Study

2022 ◽  
Author(s):  
Kokab Jabeen ◽  
Sidrah Saleem ◽  
Faiqa Arshad ◽  
Zill-e-Huma ◽  
Shah Jahan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Alternative Treatment ◽  
Therapeutic Potential ◽  
Salmonella Typhi ◽  
Drug Resistant ◽  
Manuka Honey ◽  
Extensively Drug Resistant ◽  
Alternative Treatment Option ◽  
Wide Range

Abstract Typhoid fever is a significant health problem in developing countries like Pakistan. Salmonella Typhi the causative agent of typhoid has developed resistant to almost all recommended antibiotics. Emergence of resistance to third generation cephalosporins has further complicated the situation and such strains are called as extensively drug resistant (XDR) Salmonella Typhi. Currently only available options are azithromycin and cabapenems. Recently few reports of azithromycin resistance have emerged from countries like Pakistan, India, Bangladesh and Nepal. As azithromycin is the only oral option available to treat XDR Typhoid, development of resistance may change treatment strategy altogether from out patient management to hospitalization of every patient. This may increase the burden on already weak health care system of countries like Pakistan. So there is dire need to look for the alternative treatment options. Manuka honey is well known for its therapeutic potential against wide range of bacteria including Salmonella Typhimurium. In this study 3 azithromycin resistant isolates were isolated and identified using disc diffusion, E-test and broth micro dilution methods and antibacterial activity, MIC and MBC of manuka honey was performed by agar well diffusion assay and broth micro dilution assay respectively. Manuka honey manifested significant antibacterial activity against all test isolates with zone of inhibition ranging from 7.3mm to 7.5mm, MIC and MBC values were between 10 to 15% v/v Here, we conclude that Manuka honey possess potent antibacterial activity and might be used as an alternative treatment option against azithromycin resistant XDR Typhid. However, further clinical trials are mandatory to validate our initial findings.

scholarly journals A new strategy for the green synthesis of chondroitin sulfate-reduced gold nanoparticles; in vitro evaluation of synthesized nanoparticles

Bioimpacts ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 217-226
Author(s):  
Maryam Asariha ◽  
Azam Chahardoli ◽  
Farshad Qalekhani ◽  
Mahnaz Ghowsi ◽  
Mehdi Fouladi ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Antibacterial Activity ◽  
Green Synthesis ◽  
Chondroitin Sulfate ◽  
Blood Compatibility ◽  
Spherical Shape ◽  
Hemolysis Assay ◽  
Wide Range ◽  
New Strategy

introduction: The application of gold nanoparticles (GNPs) in medicine is expanding as an effective therapeutic and diagnostic compound. Different polysaccharides with high biocompatibility and hydrophilic properties have been used for synthesis and capping of GNPs. Chondroitin sulfate (CHS) as a polysaccharide possesses a wide range of biological functions e.g. anti-oxidant, anti-inflammation, anti-coagulation, anti-atherosclerosis, anti-thrombosis with insignificant immunogenicity and has not been used for the green synthesis of GNPs. Methods: GNPs were synthesized using CHS, and their physicochemical properties were evaluated. The antibacterial activity of CHS-GNPs was estimated against both gram-positive and gram-negative bacteria. The cytotoxicity of CHS and CHS-GNPs was obtained by MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) test, and the electrocatalytic activity of CHS-GNPs was investigated. The blood compatibility was evaluated by the in vitro hemolysis assay. Results: The absorption band at 527 nm reveals the reduction of Au3+ into GNPs. The transmission electron microscopy (TEM) image displays the spherical shape of GNPs in the range of 5.8–31.4 nm. The CHS and CHS-GNPs at 300 µg/mL revealed a maximum DPPH (1, 1-diphenyl-2-picrylhydrazyl) scavenging activity of 73% and 65%, respectively. CHS-GNPs showed antibacterial activity against Bacillus subtilis, while CHS has no antibacterial activity. CHS-GNPs exhibited a cytotoxicity effect against MDA-MB-468 and βTC3 cancer cell lines, and the electrochemical study indicated a significant increase in electrocatalytic properties of CHS-GNPs coated electrode compared by the bare electrode. The hemolysis test proved the blood compatibility of CHS-GNPs. Conclusion: The results indicate the advantages of using CHS to produce blood-compatible GNPs with antioxidant, cytotoxic, and electrochemical properties.

scholarly journals Design, Development and Evaluation Of Anti-Hypertensive Drug Solid Lipid Nano Particles

2021 ◽  
Vol 11 (4) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Nano Particles ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Wide Range

Recently, solid lipid Nano-particles have received much attention by the researchers owing to its biodegradability, biocompatibility and the ability to deliver a wide range of drugs. The aim of the present study was to design Diltiazem solid lipid Nano-particles and to evaluate them. Diltiazem solid lipid Nano-particles were prepared by hot homogenization technique using different lipids (Tristearin, GMS and Comprital), soy lecithin as stabilizers and tween 80, Poloxamer as surfactants. The Nano-particles were evaluated for particle size & PDI, zeta potential, entrapment efficiency and in vitro drug release. The particle size ranged from 49.7 to 523.7 nm. PDI of all formulations were good within the range of 0.189 to 0.427. The zeta potential ranged from -10.5 to -29.6 Mv, Entrapment efficiency of all formulations were observed was in the range of 78.68 to 95.23 %. The cumulative percentage release of Diltiazem from different Diltiazem Nano-particles varied from 53.36 to 88.74% depending upon the drug lipid ratio and the type of lipid used. The average percentage of drug released from different SLNs after 24 hours showed in the following order: F9 (53.35%) < F6 (56.75%) < F4 (61.74%) < F7 (63.8%) < F5(67.77%) < F8(69.04%) < F3(75.31%) < F1(79.36%) <F2 (88.74%) respectively. The release kinetic studies showed that the release was first order diffusion controlled and the n values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Quasi-Fickian type (n-value of 0.47). Keywords: Diltiazem, solid lipid Nano-particles, FTIR, in vitro drug release.

scholarly journals DEVELOPMENT AND EVALUATION OF LYOPHILIZED POWDER TO PREPARE SOLUTION FOR INJECTIONS BASED ON DOXYCYCLINE

2021 ◽  
Vol 93 (3) ◽  
pp. 53-63
Author(s):  
E. A. Saliy ◽  
A. Yu. Honcharuk ◽  
O. V. Getalo ◽  
H. V. Tarasenko
Keyword(s):  
Solution Treatment ◽  
Parenteral Administration ◽  
Doxycycline Hyclate ◽  
Solution Ph ◽  
Long Term Storage ◽  
Accelerated Storage ◽  
Wide Range ◽  
Porous Mass

The range of doxycycline drugs on the pharmaceutical market of the Ukraine is very limited and is represented by solid forms (capsules and tablets) while a rapid effect and maximum bioavailability of the drug can be provided by parenteral administration. The object of the study is the drug doxycycline hyclate in the form of lyophilisate to prepare solution for injections. During the development of the drug it was taken into account that aqueous doxycycline solution is pH dependent and tends to shift the solution pH during long-term storage. Therefore, excipients such as stabilizer and antioxidant providing buffering properties and stability of the solution were introduced into the composition. According to the research results an optimal composition of lyophilized powder was selected, the production technology with the stage of solution treatment with activated carbon was developed which allowed to obtain lyophilized powder with a well-formed porous mass without splits, cracks and fissures, resistant to shaking, and the prepared solution for parenteral administration is stable by the «Degree of coloration» quality indicator during accelerated storage regimen. It was found that doxycycline hyclate in the form of a lyophilisate shows a wide range of antibacterial activity. Comparative studies in vitro for two drugs, in the form of lyophilisate with doxycycline hyclate for injections and hard gelatin capsules with 100 mg of doxycycline hyclate, confirm equivalence of their bacteriostatic action against bacteria causing infectious diseases in humans.

scholarly journals Rapid micropropagation, antioxidant and antibacterial assays of Ocimum spp.

2020 ◽  
Vol 49 (3) ◽  
pp. 459-465
Author(s):  
Shamoly Akter ◽  
Barna Goswami ◽  
Salim Khan ◽  
Shahina Akter ◽  
Sanjida Rahman Mollika ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Root Formation ◽  
Shoot Induction ◽  
Leaf Extracts ◽  
In Vitro Micropropagation ◽  
Wide Range ◽  
Half Strength ◽  
Ocimum Tenuiflorum ◽  
High Inhibition

In vitro micropropagation was studied in two species of Ocimum and one species was used for antioxidant and antibacterial activity. The maximum number of shoots/explant (10.1 and 9.5) was induced in MS + 1.0 mg/l BAP + 0.5 mg/l Kn and MS + 2.0 mg/l BAP + 0.5 mg/l IAA in Ocimum tenuiflorum and O. americanum, respectively. GA3 (0.1 mg/l) was found to be effective for shoot induction and elongation in both the species. Strong and stout root formation was observed on half strength MS medium supplemented with 0.2 mg/l IBA for O. tenuiflorum and half strength MS + 0.5 mg/l NAA for O. americanum. Methanolic leaf extract of O. tenuiflorum showed high inhibition of DPPH activity compared to standard antioxidants like quercetin and the chloroform leaf extracts exhibited wide range of antibacterial activity.

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