scholarly journals Targeted Propolis-Loaded Poly (Butyl) Cyanoacrylate Nanoparticles: An Alternative Drug Delivery Tool for the Treatment of Cryptococcal Meningitis

2021 ◽  
Vol 12 ◽  
Author(s):  
Patcharin Thammasit ◽  
Chayada Sitthidet Tharinjaroen ◽  
Yingmanee Tragoolpua ◽  
Volker Rickerts ◽  
Radostina Georgieva ◽  
...  
Keyword(s):  
Water Solubility ◽  
Galleria Mellonella ◽  
Cell Monolayer ◽  
Antimicrobial Properties ◽  
Toxicity Testing ◽  
Entrapment Efficiency ◽  
Normal Behavior ◽  
Alternative Drug ◽  
Invertebrate Model

In this study, we describe a nano-carrier system for propolis that is able to cross an in vitro model of the blood-brain barrier (BBB) and effectively reduce the virulence of Cryptococcus neoformans in animal models. Antimicrobial properties of propolis have been widely studied. However, propolis applications are limited by its low water solubility and poor bioavailability. Therefore, we recently formulated novel poly (n-butyl cyanoacrylate) nanoparticles (PBCA-NP) containing propolis. PBCA-NP are biocompatible, biodegradable and have been shown to effectively cross the BBB using apolipoprotein E (ApoE) as a ligand. Prepared nanoparticles were characterized for particle size, zeta potential, propolis entrapment efficiency and in vitro release. Additionally, the PBCA-NP were functionalized with polysorbate 80, which then specifically adsorbs ApoE. Using an in vitro BBB model of human brain microvascular endothelial cells hCMEC/D3, it was shown that fluorescence labelled ApoE-functionalized PBCA-NP were internalized by the cells and translocated across the cell monolayer. Propolis-loaded PBCA-NP had in vitro, antifungal activity against C. neoformans, which causes meningitis. To utilize the invertebrate model, Galleria mellonella larvae were infected with C. neoformans and treated with propolis-loaded PBCA-NP. The larvae exhibited normal behavior in toxicity testing, and treatment with propolis-loaded PBCA-NP increased survival in the C. neoformans-infected larvae group. In addition, following cryptococcal infection and then 7 days of treatment, the tissue fungal burden of mice treated with propolis-loaded PBCA-NP was significantly lower than control groups. Therefore, our ApoE-functionalized propolis-loaded PBCA-NP can be deemed as a potential targeted nanoparticle in the therapeutic treatment of cerebral cryptococcosis.

scholarly journals Development and Evaluation of Rifampicin Loaded Alginate–Gelatin Biocomposite Microfibers

Polymers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1514
Author(s):  
Ameya Sharma ◽  
Vivek Puri ◽  
Pradeep Kumar ◽  
Inderbir Singh ◽  
Kampanart Huanbutta
Keyword(s):  
Wound Healing ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Entrapment Efficiency ◽  
Tissue Proliferation ◽  
Naturally Occurring ◽  
Reinforcing Material ◽  
Vitro Release

Various systematic phases such as inflammation, tissue proliferation, and phases of remodeling characterize the process of wound healing. The natural matrix system is suggested to maintain and escalate these phases, and for that, microfibers were fabricated employing naturally occurring polymers (biopolymers) such as sodium alginate, gelatin and xanthan gum, and reinforcing material such as nanoclay was selected. The fabrication of fibers was executed with the aid of extrusion-gelation method. Rifampicin, an antibiotic, has been incorporated into a biopolymeric solution. RF1, RF2, RF3, RF4 and RF5 were coded as various formulation batches of microfibers. The microfibers were further characterized by different techniques such as SEM, DSC, XRD, and FTIR. Mechanical properties and physical evaluations such as entrapment efficiency, water uptake and in vitro release were also carried out to explain the comparative understanding of the formulation developed. The antimicrobial activity and whole blood clotting of fabricated fibers were additionally executed, hence they showed significant results, having excellent antimicrobial properties; they could be prominent carriers for wound healing applications.

scholarly journals In vitro and in vivo activity of ML302F: a thioenolate inhibitor of VIM-subfamily metallo β-lactamases

MedChemComm ◽  
2016 ◽  
Vol 7 (1) ◽  
pp. 190-193 ◽  
Author(s):  
Jonathan W. Betts ◽  
Lynette M. Phee ◽  
Muhd H. F. Abdul Momin ◽  
Klaus-Daniel Umland ◽  
Jurgen Brem ◽  
...  
Keyword(s):  
Antibiotic Susceptibility ◽  
Galleria Mellonella ◽  
Class B ◽  
Resistant Strains ◽  
Invertebrate Model ◽  
In Cells

The thioenol ML302F, recently identified as an inhibitor of class B metallo-β-lactamases (MBLs), restores antibiotic susceptibility to meropenem resistant strains in cells and the Galleria mellonella invertebrate model.

scholarly journals Enhancement and Extended Release of the Anti-hypertensive Drug Carvedilol using Optimized Ethosomal Gel via Transdermal Route

2020 ◽  
Author(s):  
Padmanabha Rao Amarachinta ◽  
Noufel Samed ◽  
Ananda Kumar Ch. ◽  
Madhusudhan Alle ◽  
Jin-Chul Kim
Keyword(s):  
Drug Release ◽  
Transdermal Delivery ◽  
Physical Appearance ◽  
Entrapment Efficiency ◽  
Hepatic Metabolism ◽  
In Vitro Drug Release ◽  
Rapid Action ◽  
Alternative Drug ◽  
Hypertensive Drug

Abstract BackgroundCarvedilol, a popular anti-hypertensive drug, when orally administered has very poor bioavailability on the account of undergoing hepatic metabolism and therefore it becomes primal to explore an alternative drug delivery route for carvedilol. For a drug to be delivered by undergoing the least number of stages of metabolism and achieve high target specificity, transdermal delivery is the most preferred route. Hence, a study was conducted to test the potential of ethosomes as a candidate for transdermal delivery of carvedilol. A statistical study by using Central Composite Design (CCD) was also conducted for optimizing the quantity of the primary constituents present in the ethosomes. The optimized ethosomal formulation was then incorporated into a hydrogel to prepare the ethosomal gel.ResultsThe optimized formulated ethosomal suspension and the ethosomal gel were undergone physicochemical, compatibility and in-vitro drug release studies along with characterization studies. The incorporation of the ethosomes into the hydrogel proved to be effective for skin application thereby ensuring better transdermal delivery. The optimized ethosomal gel has showed credible physical appearance, spreadability, viscosity and in-vitro drug release. The pharmacodynamic studies conducted on Wister rats revealed that the anti-hypertensive action was gradual and sustained lasting up to a period of 24 hours. The stability studies conducted also showed that prepared formulations maintained its consistency within the range for the measured parameters of physical appearance, rheological properties and entrapment efficiency for a period of 3 months.Conclusions The incorporation of the drug loaded into hydrogel and its effect on regulating systolic blood pressure in a sustained way lasting 24 hours proved to be better than the present available marketed formulation which has a rapid action with the anti-hypertensive effect lasting only for 10 hours. The chosen route for delivering the drug transdermally hence proved to be effective with better enhancement and permeation capability and shows the high potential of ethosomes to be considered for novel delivery of other anti-hypertensive drugs.

Preparation and Characterization of PEGylated Iron Oxide-Gold Nanoparticles for Delivery of Sulforaphane and Curcumin

Drug Research ◽  
2017 ◽  
Vol 67 (12) ◽  
pp. 698-704 ◽  
Author(s):  
Hossein Danafar ◽  
Ali Sharafi ◽  
Sonia Askarlou ◽  
Hamidreza Manjili
Keyword(s):  
Cell Line ◽  
Water Solubility ◽  
Drug Loading ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Breast Adenocarcinoma ◽  
Therapeutic Effects ◽  
Loading Capacity ◽  
Au Nps

AbstractNatural products have been used for the treatment of various diseases such as cancer. Curcumin (CUR) and sulforaphane (SF) have anti-cancer effects, but their application is restricted because of their low water solubility and poor oral bioavailability. To improve the bioavailability and solubility of SF and CUR, we performed an advanced delivery of SF and CUR with PEGylated gold coated Fe3O4 magnetic nanoparticles (PEGylated Fe3O4@Au NPs) to endorse SF and CUR maintenance as an effective and promising antitumor drugs. The structure of the synthesized nanocarrieris evaluated by, transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FT-IR). The results revealed that the size of NPs was 20 nm. They were mono-dispersed in water, with high drug-loading capacity and stability. CUR and SF were encapsulated into NPs with loading capacity of 16.32±0.023% and 15.74±0.015% and entrapment efficiency of 74.57±0.14% and 72.20±0.18% respectively. The in-vitro study of SF and CUR loaded PEGylated Fe3O4@Au NPs on human breast adenocarcinoma cell line (SK-BR-3) confirmed that cytotoxicity of SF and CUR can enhance when they are loaded on PEGylated Fe3O4@Au NPs in comparison to Free SF and void CUR. The results of flow cytometry and real-time PCR shown that nano-carriers can increase therapeutic effects of SF and CUR by apoptosis and necrosis induction as well as inhibiting of migration in SK-BR-3 cell line.

scholarly journals Enhancement Solubilization of Dutasteride using Microsponge Formulation

2020 ◽  
Vol 10 (01) ◽  
pp. 60-67
Author(s):  
Hassanien S. Taghi ◽  
Mustafa R. Abdulbaqi ◽  
Esraa G. Jabar
Keyword(s):  
Particle Size ◽  
Physical Properties ◽  
Water Solubility ◽  
Oral Absorption ◽  
Entrapment Efficiency ◽  
Production Yield ◽  
Internal Surface Area ◽  
Prostate Hyperplasia ◽  
Saturated Solubility

Dutasteride (DU) (5α-reductase inhibitor) that is used for the treatment of benign prostate hyperplasia (BPH), DU has low water solubility and poor oral absorption that classified as Biopharmaceutics Classification System (BCS) class II. This study aims to improve the physical properties of Dutasteride (DU) like solubility by the preparation of microsponge (MS). Microsponges are spherical in shape, sponge-like structure, polymeric delivery systems composed of porous microspheres with a large internal surface area. Nine formulations of DU MS had been prepared by the technique of quasi-emulsion solvent diffusion (QESD) and utilizing Eudragit S100 as major polymer and glycerol as a plasticizer that dissolved in dichloromethane where polyvinyl alcohol PVA serves as a stabilizer in the external phase. The formulas were employed to optimize preparation variable factors include; different drug to polymer ratio, the addition of different concentrations of PVA, and stirring rate. Optimization was done using the response of production yield (PY), entrapment efficiency EE), particle size, and in vitro drug release; The results display that the best ratio of (drug: polymer) was 5:1, and the best rate of stirring was 1,000 rpm respecting the optimum characteristics of microsponge. The best-selected formula prepared (F2) was underwent to evaluation regarding saturated solubility, FTIR, DSC, and SEM and showed 1.28 folds enhancement in saturated solubility compared to plain DU, and was well fabricated with high entrapment efficiency (83.7% ± 1.37), production yield (85.61% ± 0.6), and particle size of 77μm. Moreover, the percent release of DU was 75.74 ± 1.5 after 4 hours, with good compatibility as confirmed by XRD, SEM, DSC, and fourier-transform infrared spectroscopy (FTIR) analysis. It can be concluded that the selected formula prepared (F2) of DU microsponge is reassuring and promising drug delivery with improved pharmaceutical physical properties.

scholarly journals Optimization of entrapment efficiency and release of clindamycin in microsponge based gel

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
ALAA KHATTAB ◽  
Abdulhakim Nattouf
Keyword(s):  
Water Solubility ◽  
Entrapment Efficiency ◽  
Physical Characterization ◽  
Diffusion Method ◽  
Free Base ◽  
Scanning Calorimetry ◽  
External Phase ◽  
Microscopy Images ◽  
Emulsion Solvent Diffusion Method

AbstractThe aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conversion of the hydrochloride salt to free base was done. By using an emulsion solvent diffusion method, we made six different formulations of microsponges containing CLN-free base by changing the proportions of polymer, emulsifier and the pH of the external phase. These formulations were studied for physical characterization and for drug- polymer interactions. The physical characterization showed that microsponge formulations coded by C5, C6 resulted in a better loading efficiency and production yield and their particle size was less than 30 µm. Scanning electron microscopy images showed the microsponges porous and spherical. C5, C6 microsponge formulation was prepared as gel in Carbopol and in vitro evaluated. The microsponge formulation gel C8 was found to be optimized. C8 released 90.38% of drug over 12 h and showed viscosity 20,157 ± 38 cp, pH of 6.3 ± 0.09 and drug content of 99.64 ± 0.04%. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed no significant interactions between excipients and drug.

scholarly journals CUR-CA-THIONE: A NOVEL CURCUMIN CONCOCTION WITH ENHANCED WATER SOLUBILITY AND BRAIN BIO-AVAILABILITY

2016 ◽  
Vol 8 (12) ◽  
pp. 265 ◽  
Author(s):  
Devang Y. Shelat ◽  
Sanjeev R Acharya
Keyword(s):  
Wistar Rats ◽  
Water Solubility ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Systemic Circulation ◽  
Oral Route ◽  
Male Wistar Rats ◽  
Dialysis Bag

<p><strong>Objective: </strong>Curcumin, is widely studied as a potential drug in treating various disorders but lacks applicability due to poor water solubility and tissue bioavailability. The main objective of the study was to develop a formulation of curcumin that has enhanced water solubility and brain bioavailability.</p><p><strong>Methods: </strong>A curcumin concoction was prepared using solvent evaporation technique taking casein and glutathione as vectors. Various process parameters were identified namely time, temperature, pH and vector while formulation parameters included drug entrapment, anti-oxidant activity, and water solubility. The concoctions were evaluated for <em>in vitro</em> release kinetics at three pH i.e. 1.2, 4.5 and 6.2 at six-time intervals i.e. 10, 20, 30, 40, 60, 120 min using dialysis bag membrane. The same kinetics was further validated using same time points with wistar rats and giving concoction at a single dose of 2 g/kg via the oral route.</p><p><strong>Results: </strong>A concoction i.e. CUR-CA-THIONE having significant entrapment efficiency (77.83%, 97.75%, 90.19%), water solubility (40, 350 and 45 times than normal curcumin) and DPPH activity (IC<sub>50</sub>: 28.91, 25.07 and 27.89) was evaluated in concoctions CUR-CA-THIONE-T.1, CUR-CA-THIONE-T.2 and CUR-CA-THIONE-T.3 respectively. These formulations were then carried out for <em>in vitro</em> release profile at different pH with average release obtained between 20-30 min. <em>In vivo</em> kinetics was studied by isolating tissues like brain, liver, lung, kidney and spleen in male wistar rats and maximum brain bioavailability was observed for CUR-CA-THIONE-T.3 at 30 min with 75 ng/g of brain tissue.</p><p><strong>Conclusion: </strong>The experiment helps in concluding that CUR-CA-THIONE has improved its water solubility and is able to by-pass systemic circulation to targeted activity.</p>

Development, In Vitro Characterization, Antitumor and Aerosol Performance Evaluation of Respirable Prepared by Self-nanoemulsification Method

Drug Research ◽  
2017 ◽  
Vol 67 (06) ◽  
pp. 343-348 ◽  
Author(s):  
Neda Naseri ◽  
Parvin Zakeri-Milani ◽  
Hamed Hamishehkar ◽  
Younes Pilehvar-Soltanahmadi ◽  
Hadi Valizadeh
Keyword(s):  
Water Solubility ◽  
Entrapment Efficiency ◽  
Dry Powder ◽  
Dry Powders ◽  
In Vitro Characterization ◽  
Lung Cancer Therapy ◽  
Development In Vitro ◽  
Next Generation Impactor ◽  
Spray Dried

AbstractPoor water solubility and low oral bioavailability limit the clinical application of Erlotinib as an anticancer. For this purpose, we encapsulated erlotinib in the solid lipid nanoparticles (SLN) and designed a spray-dried dry powder inhalable (DPI) formulation. Erlotinib-loaded SLNs were prepared using self-nanoemulsifying and characterized for physicochemical properties. Pulmonary deposition of spray-dried DPI formulation was performed using Next Generation Impactor. The particle size and zeta potential of Erlotinib-loaded SLNs were 300 to 800 nm and −18 to −32 mV, respectively. High drug entrapment efficiency in the narrow range of 80–85% was achieved. Cytotoxicity results indicated that cell growth inhibition of free drug and drug loaded nanoparticles is dose- and time-dependent. Inhalable dry powders prepared from drug-loaded SLNs were found to have a fine particle fraction in the range of 6.92±0.99 –11.24±2.4%, mean mass aerodynamic diameter in the range of 4.52±0.1 to 6.67±0.5 µm. The findings revealed that the proposed inhalable dry powder formulation loaded with erlotinib SLN has potential in lung cancer therapy through pulmonary route.

scholarly journals Adenylate Kinase Release as a High-Throughput-Screening-Compatible Reporter of Bacterial Lysis for Identification of Antibacterial Agents

2012 ◽  
Vol 57 (1) ◽  
pp. 26-36 ◽  
Author(s):  
Anna C. Jacobs ◽  
Louis DiDone ◽  
Jennielle Jobson ◽  
Madeline K. Sofia ◽  
Damian Krysan ◽  
...  
Keyword(s):  
Adenylate Kinase ◽  
High Throughput Screening ◽  
Antimicrobial Agents ◽  
Galleria Mellonella ◽  
Bacterial Species ◽  
Antimicrobial Properties ◽  
Infection Model ◽  
Intracellular Enzyme ◽  
Content Type

ABSTRACTAdenylate kinase (AK) is a ubiquitous intracellular enzyme that is released into the extracellular space upon cell lysis. We have shown that AK release serves as a useful reporter of bactericidal agent activity and can be exploited for antimicrobial screening purposes. The AK assay exhibits improved sensitivity over that of growth-based assays and can detect agents that are active against bacteria in clinically relevant growth states that are difficult to screen using conventional approaches, such as small colony variants (SCV) and bacteria within established biofilms. The usefulness of the AK assay was validated by screening a library of off-patent drugs for agents that exhibit antimicrobial properties toward a variety of bacterial species, includingEscherichia coliand all members of the “ESKAPE” pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacterspecies). The assay detected antibiotics within the library that were expected to be active against the organism screened. Moreover, 38 drugs with no previously reported antibacterial activity elicited AK release. Four of these were acquired, and all were verified to exhibit antimicrobial activity by standard susceptibility testing. Two of these molecules were further characterized. The antihistamine, terfenadine, was active againstS. aureusplanktonic, SCV population, and biofilm-associated cells. Tamoxifen, an estrogen receptor antagonist, was active towardE. faeciumin vitroand also reducedE. faeciumpathogenesis in aGalleria mellonellainfection model. Our data demonstrate that the AK assay provides an attractive screening approach for identifying new antimicrobial agents. Further, terfenadine and tamoxifen may represent novel antimicrobial drug development scaffolds.

scholarly journals Preparation and In vitro Evaluation of Isoniazid-Containing Dex-HEMA-Co-PNIPAAm Nanogels

2015 ◽  
Vol 37 ◽  
pp. 55 ◽  
Author(s):  
Maryam Jafari ◽  
Babak Kaffashi
Keyword(s):  
Drug Loading ◽  
Antimicrobial Properties ◽  
Entrapment Efficiency ◽  
Loading Capacity ◽  
In Vitro Drug Release ◽  
E Coli ◽  
Toxic Product ◽  
Good Biocompatibility ◽  
Characteristic Features

In this work, Dex-HEMA-Co-PNIPAAm nanogels containing Isoniazid antibiotic were made. Characteristic features of nanogels were studied by Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS) and scanning electron microscopy (SEM). Drug loading capacity and entrapment efficiency were determined. In vitro drug release amount was estimated at room and body temperature. Biocompatibility of gels was investigated through cytotoxicity assay. Finally antimicrobial properties of synthesized gels were studied. It was shown from the experimental data that the nanogels size after drug loading increased about 1-2%. %Isoniazid loading and %entrapment efficiency were in the range of 15-22% and 37-48% respectively. After 10 days of degradation ca. 80% at 25ºC and ca. 90% at 37ºC of the nanogel structures were destructed. No significant toxic product produced while degradation and all nanogels depicted good biocompatibility. No antimicrobial features observed through the test condition against gram negative E Coli.

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