scholarly journals Development of Provesicular Nanodelivery System of Curcumin as a Safe and Effective Antiviral Agent: Statistical Optimization, In Vitro Characterization, and Antiviral Effectiveness

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5668
Author(s):  
Farid A. Badria ◽  
Abdelaziz E. Abdelaziz ◽  
Amira H. Hassan ◽  
Abdullah A. Elgazar ◽  
Eman A. Mazyed
Keyword(s):  
Antiviral Agent ◽  
Entrapment Efficiency ◽  
Docking Study ◽  
In Vitro Characterization ◽  
Slurry Method ◽  
32 Factorial Design ◽  
Simplex Virus ◽  
The Impact ◽  
Low Solubility

Curcumin is a natural compound that has many medical applications. However, its low solubility and poor stability could impede its clinical applications. The present study aimed to formulate dry proniosomes to overcome these pitfalls and improve the therapeutic efficacy of Curcumin. Curcumin-loaded proniosomes were fabricated by the slurry method according to 32 factorial design using Design-Expert software to demonstrate the impact of different independent variables on entrapment efficiency (EE%) and % drug released after 12 h (Q12h). The optimized formula (F5) was selected according to the desirability criteria. F5 exhibited good flowability and appeared, after reconstitution, as spherical nanovesicles with EE% of 89.94 ± 2.31% and Q12h of 70.89 ± 1.62%. F5 demonstrated higher stability and a significant enhancement of Q12h than the corresponding niosomes. The docking study investigated the ability of Curcumin to bind effectively with the active site of DNA polymerase of Herpes simplex virus (HSV). The antiviral activity and the safety of F5 were significantly higher than Curcumin. F5 improved the safety of Acyclovir (ACV) and reduced its effective dose that produced a 100% reduction of viral plaques. Proniosomes could be promising stable carriers of Curcumin to be used as a safe and efficient antiviral agent.

scholarly journals Diacerein-Loaded Hyaluosomes as a Dual-Function Platform for Osteoarthritis Management via Intra-Articular Injection: In Vitro Characterization and In Vivo Assessment in a Rat Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 765
Author(s):  
Nouran O. Abdelmageed ◽  
Nadia M. Morsi ◽  
Rehab N. Shamma
Keyword(s):  
Hyaluronic Acid ◽  
Cartilage Damage ◽  
Entrapment Efficiency ◽  
Dual Function ◽  
In Vitro Characterization ◽  
Drug Entrapment Efficiency ◽  
Formulation Parameters ◽  
Acid Gel

The application of intra-articular injections in osteoarthritis management has gained great attention lately. In this work, novel intra-articular injectable hyaluronic acid gel-core vesicles (hyaluosomes) loaded with diacerein (DCN), a structural modifying osteoarthritis drug, were developed. A full factorial design was employed to study the effect of different formulation parameters on the drug entrapment efficiency, particle size, and zeta potential. Results showed that the prepared optimized DCN- loaded hyaluosomes were able to achieve high entrapment (90.7%) with a small size (310 nm). The morphology of the optimized hyaluosomes was further examined using TEM, and revealed spherical shaped vesicles with hyaluronic acid in the core. Furthermore, the ability of the prepared DCN-loaded hyaluosomes to improve the in vivo inflammatory condition, and deterioration of cartilage in rats (injected with antigen to induce arthritis) following intra-articular injection was assessed, and revealed superior function on preventing cartilage damage, and inflammation. The inflammatory activity assessed by measuring the rat’s plasma TNF-α and IL-1b levels, revealed significant elevation in the untreated group as compared to the treated groups. The obtained results show that the prepared DCN-loaded hyaluosomes would represent a step forward in the design of novel intra articular injection for management of osteoarthritis.

scholarly journals Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 465 ◽  
Author(s):  
Eman A. Mazyed ◽  
Abdelaziz E. Abdelaziz
Keyword(s):  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Ocular Delivery ◽  
Ethanol Injection ◽  
In Vitro Characterization ◽  
Span 60 ◽  
In Vivo Characterization

Acetazolamide (ACZ) is a potent carbonic anhydrase inhibitor that is used for the treatment of glaucoma. Its oral administration causes various undesirable side effects. This study aimed to formulate transgelosomes (TGS) for enhancing the ocular delivery of ACZ. ACZ-loaded transfersomes were formulated by the ethanol injection method, using phosphatidylcholine (PC) and different edge activators, including Tween 80, Span 60, and Cremophor RH 40. The effects of the ratio of lipid to surfactant and type of surfactant on % drug released after 8 h (Q8h) and entrapment efficiency (EE%) were investigated by using Design-Expert software. The optimized formula was formulated as TGS, using poloxamers as gelling agents. In vitro and in vivo characterization of ACZ-loaded TGS was performed. According to optimization study, F8 had the highest desirability value and was chosen as the optimized formula for preparing TGS. F8 appeared as spherical elastic nanovesicles with Q8h of 93.01 ± 3.76% and EE% of 84.44 ± 2.82. Compared to a free drug, TGS exhibited more prolonged drug release of 71.28 ± 0.46% after 8 h, higher ex vivo permeation of 66.82 ± 1.11% after 8 h and a significant lowering of intraocular pressure (IOP) for 24 h. Therefore, TGS provided a promising technique for improving the corneal delivery of ACZ.

scholarly journals The BioGIT System: a Valuable In Vitro Tool to Assess the Impact of Dose and Formulation on Early Exposure to Low Solubility Drugs After Oral Administration

2018 ◽  
Vol 20 (4) ◽  
Author(s):  
Alexandros Kourentas ◽  
Maria Vertzoni ◽  
Vicky Barmpatsalou ◽  
Patrick Augustijns ◽  
Stefania Beato ◽  
...  
Keyword(s):  
Oral Administration ◽  
Early Exposure ◽  
System A ◽  
The Impact ◽  
Low Solubility ◽  
Low Solubility Drugs

A Logical Approach to Development of Natamycin Loaded NLCs: Preformulation Studies, Formulation Development and In Vitro Characterization

2021 ◽  
pp. 6033-6040
Author(s):  
Ishwari Choudhary ◽  
Preeti K. Suresh
Keyword(s):  
Entrapment Efficiency ◽  
Formulation Development ◽  
Visible Spectroscopy ◽  
Scanning Calorimetry ◽  
Solubility Profile ◽  
In Vitro Characterization ◽  
Uv Visible ◽  
Preformulation Studies

This study was aimed at the development of natamycin loaded nano-structured lipid carriers (NLCs) and their characterization for physicochemical properties i.e., Fourier Transform Infrared (FTIR), UV-Visible spectroscopy, meting point, solubility profile and partition coefficient. FTIR and Differential Scanning Calorimetry (DSC) permit the characterization of the drug, excipients and binary mixture and thus assisted in predicting the compatibility of natamycin with other excipients. Lipid screening for formulation of NLCs were performed by their solubility and drug affinity studies. High homogenization and sonication method was employed for the development of natamycin loaded NLCs and it was characterized for vesicle size, zeta potential, % entrapment efficiency, viscosity, pH and percentage drug release up to 12 h.

BOX–BEHNKEN METHOD TO OPTIMIZE LORNOXICAM PRONIOSOMES: PREPARATION, IN VITRO CHARACTERIZATION AND ANALGESIC ACTIVITY

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (06) ◽  
pp. 21-33
Author(s):  
K. Vijaya Sri ◽  
◽  
D. Sandhya ◽  
M. Manchala ◽  
R. S Dashamukhi
Keyword(s):  
Analgesic Effect ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Factors Affecting ◽  
Drug Diffusion ◽  
Percutaneous Permeation ◽  
In Vitro Characterization ◽  
Diffusion Studies ◽  
Drug Entrapment Efficiency

The objective of present investigation was to develop and evaluation of proniosomes as the carrier of lornoxicam for topical delivery. lornoxicam-loaded proniosomes were prepared by coacervation phase separation method. The Box–Behnken design used in this study helped in identifying the factors affecting drug entrapment efficiency and drug diffusion. Proniosomes were evaluated for appearance, pH, viscosity, entrapment efficiency and in vitro drug diffusion studies. The optimized formulations were further evaluated to vesicle size, shape, zeta potential, percutaneous permeation and analgesic effect. The vesicles were found to be unilamellar, spherical in shape. The analgesic effect of lornoxicam proniosomal gel showed better therapeutic activity.

scholarly journals The Antiviral Agent Hypericin has in vitro Activity against HSV-1 Through Non-Specific Association with Viral and Cellular Membranes

1994 ◽  
Vol 5 (2) ◽  
pp. 83-90 ◽  
Author(s):  
N. D. Weber ◽  
B. K. Murray ◽  
J. A. North ◽  
S. G. Wood
Keyword(s):  
Antiviral Agent ◽  
Vero Cells ◽  
Yield Reduction ◽  
Fluorescence Studies ◽  
Cytoplasmic Membranes ◽  
Specific Affinity ◽  
Specific Association ◽  
Simplex Virus ◽  
Hsv 1

The antiviral and virucidal compound, hypericin, was studied regarding its activity and possible mechanism against herpes simplex virus (HSV-1). It was determined that hypericin caused slight inhibition of viral adsorption to and penetration of Vero cells. Additionally, yield reduction assays suggested that hypericin was most effective against HSV-1 as a virucidal agent rather than as an intracellular antiviral agent. Fluorescence microscopy revealed that hypericin initially associated with cytoplasmic membranes and that over the course of time it became concentrated in intracellular membranous regions, probably the Golgi apparatus or endoplasmic reticulum (ER). These concentration events failed to inhibit glycosylation of either viral or cellular proteins and were effectively blocked by compounds which inhibit endocytosis or membrane cycling between the ER and Golgi. Based on fluorescence studies, it was determined that hypericin had non-specific affinity for protein and higher affinity for detergent and lipid. The evidence suggested that strong, non-specific association with membranes, both viral and cellular, are probably the basis of hypericin's virucidal and antiviral activity.

scholarly journals Drug Susceptibility and Replicative Capacity of Multidrug-Resistant Recombinant Human Cytomegalovirus Harboring Mutations in UL56 and UL54 Genes

2017 ◽  
Vol 61 (11) ◽  
Author(s):  
Jocelyne Piret ◽  
Nathalie Goyette ◽  
Guy Boivin
Keyword(s):  
Human Cytomegalovirus ◽  
Double Mutant ◽  
Antiviral Agent ◽  
Drug Susceptibility ◽  
Multidrug Resistant ◽  
Wild Type Virus ◽  
Replicative Capacity ◽  
Wild Type ◽  
The Impact

ABSTRACT Letermovir is an investigational antiviral agent with a novel mechanism of action involving the viral terminase (pUL56). We evaluated the impact of the V236M mutation in the UL56 gene alone and in combination with the E756K mutation in the UL54 gene on drug susceptibility and viral replicative capacity of recombinant human cytomegalovirus. The double mutant exhibited at least borderline resistance to all antivirals tested (ganciclovir, foscarnet, cidofovir, brincidofovir, and letermovir) and replicated less efficiently than the wild-type virus in vitro.

Synthesis of 5-(1-azidovinyl) and 5-[2-(1-azirinyl)] analogs of 2′-deoxyuridine

1996 ◽  
Vol 74 (9) ◽  
pp. 1609-1615 ◽  
Author(s):  
Rakesh Kumar ◽  
Leonard I. Wiebe ◽  
Edward E. Knaus
Keyword(s):  
Thermal Decomposition ◽  
Herpes Simplex ◽  
Mortality Rate ◽  
Antiviral Agent ◽  
Varizella Zoster Virus ◽  
Antiviral Activities ◽  
Simplex Virus ◽  
Hsv 1

The regiospecific addition of bromine azide to the vinyl substituent of 5-vinyl-3′,5′-di-O-acetyl- (or tert-butyldimethylsilyl)-2′-deoxyuridines (2) yielded the corresponding 5-(1-azido-2-bromoethyl)-3′,5′-di-O-protected-2′-deoxyuridines (3). Treatment of the 5-(1-azido-2-bromoethyl) compounds 3 with t-BuOK, to effect the base-catalyzed elimination of HBr, afforded the corresponding 5-(1-azidovinyl)-2′-deoxyuridines (4, 7). Thermal decomposition of 5-(1-azidovinyl)-2′-deoxyuridine (7) at 110 °C in dioxane yielded 5-[2-(1 -azirinyl)]-2′-deoxyuridine (9). 5-(1 -Azidovinyl)-2′-deoxyuridine (7) exhibited appreciable in vitro antiviral activities againist herpes simplex virus type 1 (HSV-1) and varizella zoster virus (VZV). Athough 7 increased the length of survival of HSV-1 brain-infected mice, it did not decrease the mortality rate relative to placebo. 5-[2-(1-Azirinyl)]-2′-deoxyuridine (9) was an inactive antiviral agent. Key words: azidovinyl, azirinyl, 2′-deoxyuridine, antiviral activity.

Sign in / Sign up

Export Citation Format

Share Document