ABSTRACT
Ethnopharmacological relevance of Saussurea species for anti-cancer compounds instigated us to develop chemotherapeutic herbal tablets. This study was an ongoing part of our previous research based on the scientific evaluation of Saussurea heteromalla (S. heteromalla) for anti-cancer lead compounds. In the current study, S. heteromalla herbal tablets (500 /800 mg) were designed and evaluated for anti-cancer activity. Arctigenin was found as a bioactive lead molecule with anti-cancer potential for cervical cancer. The in vitro results on the HeLa cell line supported the ethnopharmacological relevance and traditional utilization of S. heteromalla and provided the scientific basis for the management of cervical cancer as proclaimed by traditional practitioners in China. LD50 of the crude extract was established trough oral acute toxicity profiling in mice, wherein the minimum lethal dose was noticed as higher than 1000 mg/kg body weight orally. Chromatographic fingerprint analysis ensured the identity and consistency of S. heteromalla in herbal tablets in terms of standardization of the herbal drug. About 99.15% of the drug (S. heteromalla crude extract) was recovered in herbal tablets (RSD: 0.45%). In vitro drug release profile was found to be more than 87% within 1 h, which was also correlated with different mathematical kinetic models of drug release (r2 = 0.992), indicating that drug release from matrix tablets into the blood is constant throughout the delivery. The dosage form was found stable after an accelerated stability parameters study which may be used for anti-cervical cancer therapy in the future, if it qualifies successful preclinical investigation parameters.
Subject(s)
Plant Extracts , Saussurea , Saussurea/chemistry , Animals , Humans , Mice , HeLa Cells , Plant Extracts/chemistry , Plant Extracts/toxicity , Plant Extracts/pharmacology , Lignans/pharmacology , Lignans/chemistry , Female , Furans/toxicity , Furans/chemistry , Furans/pharmacology , Tablets , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Male , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Lethal Dose 50 , Toxicity Tests, Acute , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/toxicity , Drugs, Chinese Herbal/pharmacologyABSTRACT
Nanotechnology has emerged as the eminent focus of today's research to overcome challenges related to conventional drug delivery systems. A wide spectrum of novel delivery systems has been investigated to improve the therapeutic outcomes of drugs. The polymer-based nanocomposite hydrogels (NCHs) that have evolved as efficient carriers for controlled drug delivery are of particular interest in this regard. Nanocomposites amalgamate the properties of both nanoparticles (NPs) as well as hydrogels, exhibiting superior functionalities over conventional hydrogels. This multiple functionality is based upon advanced mechanical, electrical, optical as well as magnetic properties. Here is a brief overview of the various types of nanocomposites, such as NCHs based on Carbon-bearing nanomaterials, polymeric nanoparticles, inorganic nanoparticles, and metal and metal-oxide NPs. Accordingly, this article will review numerous ways of preparing these NCHs with particular emphasis on the vast biomedical applications displayed by them in numerous fields such as tissue engineering, drug delivery, wound healing, bioprinting, biosensing, imaging and gene silencing, cancer therapy, antibacterial therapy, etc. Moreover, various features can be tuned, based on the final application, by controlling the chemical composition of hydrogel network, which may also influence the released conduct. Subsequently, the recent work and future prospects of this newly emerging class of drug delivery system have been enlisted.
Subject(s)
Drug Delivery Systems , Polymers , Humans , Nanogels , Biological Availability , Polymers/chemistry , Hydrogels/chemistryABSTRACT
The primary objective of this study was to assess the potential utility of quince seed mucilage as an excipient within a graft copolymer for the development of an oral-controlled drug delivery system. The Cydonia oblonga-mucilage-based graft copolymer was synthesized via a free radical polymerization method, employing potassium per sulfate (KPS) as the initiator and N, N-methylene bisacrylamide (MBA) as the crosslinker. Various concentrations of monomers, namely acrylic acid (AA) and methacrylic acid (MAA), were used in the graft copolymerization process. Metoprolol tartarate was then incorporated into this graft copolymer matrix, and the resultant drug delivery system was subjected to comprehensive characterization using techniques such as Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The swelling behavior of the drug delivery system was evaluated under different pH conditions, and in vitro drug release studies were conducted. Furthermore, pharmacokinetic parameters including the area under the curve (AUC), maximum plasma concentration (Cmax), time to reach Cmax (Tmax), and half-life (t1/2) were determined for metoprolol-loaded hydrogel formulations in rabbit plasma, and these results were compared with those obtained from a commercially available product. The key findings from the study include observations that higher concentrations of acrylic acid (AA) and Cydonia oblonga mucilage (CM) in the graft copolymer enhanced swelling, while the opposite trend was noted at elevated concentrations of methacrylic acid (MAA) and N, N-methylene bisacrylamide (MBA). FTIR analysis confirmed the formation of the graft copolymer and established the compatibility between the drug and the polymer. SEM imaging revealed a porous structure in the prepared formulations. Additionally, the swelling behavior and drug release profiles indicated a pH-sensitive pattern. The pharmacokinetic assessment revealed sustained release patterns of metoprolol from the hydrogel network system. Notably, the drug-loaded formulation exhibited a higher Cmax (156.48 ng/mL) compared to the marketed metoprolol product (96 ng/mL), and the AUC of the hydrogel-loaded metoprolol was 2.3 times greater than that of the marketed formulation. In conclusion, this study underscores the potential of quince seed mucilage as an intelligent material for graft-copolymer-based oral-controlled release drug delivery systems.
ABSTRACT
Prime objective of the current research was to develop a stable nimesulide emulgel with the help of arabinoxylan, a natural gelling agent extracted from Plantago ovata. The response surface methodology was used by a Design Expert 10 software to formulate and optimize the emulgel. The experimental design approach evaluated the impact of independent and dependent variables. Independent variables were different concentrations of arabinoxylan, span 80 and tween 20, whereas, dependent variables were viscosity, pH, and content uniformity. FTIR demonstrated the compatibility of nimesulide with the excipients. Stability study indicated no phase separation and no change in pH for formulation F1, F3 and F4. The negative values of zeta potential revealed the excellent stability of emulgel. Viscosity, spreadability and extrudability values were in desired range. Ex-vivo permeation study illustrated 86%, 55% and 66% release of the drug over a period of 24 h from the formulations F1, F3 and F4, respectively. Analgesic effect of the optimized emulgel was significantly higher in test group as compared to control and did not produce any sort of irritation. Therefore, it can be concluded that the newly developed emulgel based on arabinoxylan, as gelling agent, appear to be an effective drug delivery system.
Subject(s)
Plantago , Excipients , Cell Movement , GelsABSTRACT
A hydrogel topical patch of neomycin was developed by using sodium alginate (SA) and hydroxyethylcellulose (HEC) as polymers. Free radical polymerization in an aqueous medium was initiated by using acrylic acid (AA) and N,N'-methylenebisacrylamide (MBA). Prepared hydrogels were characterized for pH sensitivity and sol-gel analysis. In addition, the effect of reactant contents on the developed formulation was evaluated by swelling behavior. SEM assay showed the rough structure of the hydrogel-based polymeric matrix, which directly enhances the ability to uptake fluid. FTIR spectra revealed the formation of a new polymeric network between reactant contents. TGA and DSC verified that fabricated polymeric patches were more thermodynamically stable than pure components. Gel fractions increased with increases in polymer, monomer, and cross-linker contents. The swelling study showed the pH-dependent swelling behavior of patches at pH 5.5, 6.5, and 7.4. The release pattern of the drug followed zero-order kinetics, with diffusion-controlled drug release patterns according to the Korsmeyer-Peppas (KP) model. Ex vivo studies across excised rabbit skin verified the drug retention in the skin layers. The hydrogel patch effectively healed the wounds produced on the rabbit skin, whereas the formulation showed no sign of irritation on intact skin. Therefore, neomycin hydrogel patches can be a potential candidate for controlled delivery for efficient wound healing.
ABSTRACT
The present study was conducted to fabricate and characterize mucilage-based polymeric networks of Aloe vera for controlled drug release. Aloe vera mucilage was used to develop a polymeric network via the free-radical polymerization method using potassium persulphate as the initiator, N' N'-Methylene bisacrylamide as the crosslinker, and acrylamide as the monomer. Using varying concentrations of Aloe vera mucilage, crosslinker, and monomer, we developed different formulations. Swelling studies were conducted at pH 1.2 and 7.4. Concentrations of polymer, monomer, and crosslinker were optimized as a function of swelling. Porosity and gel content were calculated for all samples. FTIR, SEM, XRD, TGA, and DSC studies were conducted for the characterization of polymeric networks. Thiocolchicoside was used as a model drug to study the in vitro release in acidic and alkaline pH. Various kinetics models were applied by using a DD solver. Increasing content of monomer and crosslinker swelling, porosity, and drug release decreased while gel content increased. An increase in Aloe vera mucilage concentration promotes swelling, porosity, and drug release of the polymeric network but decreases gel content. The FTIR study confirmed the formation of crosslinked networks. SEM indicated that the polymeric network had a porous structure. DSC and XRD studies indicated the entrapment of drugs inside the polymeric networks in amorphous form. The analytical method was validated according to ICH guidelines in terms of linearity, range, LOD, LOQ, accuracy, precision, and robustness. Analysis of drug release mechanism revealed Fickian behavior of all formulations. All these results indicated that the M1 formulation was considered to be the best polymeric network formulation in terms of sustaining drug release patterns.
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Present study was carried out to analyze the impact of three different monomers on release of losartan potassium from graft polymeric network prepared through free radical polymerization. N, N-methylene bis acrylamide was used as crosslinker and potassium persulfate as initiator. Losartan potassium as used as model drug because, it has very small plasma half-life and wide range of applications as an effective and efficient ARB (Angiotensin II Receptor Blockers) causing lower incidence of side - effects. Influence of three different monomers on swelling and in vitro drug release of the delivery system was evaluated at pH 1.2 and 7.4. The polymeric networks were characterized by Fourier transform infrared spectroscopy, Thermogravimetric analysis and Scanning electron microscopy. Polymeric network prepared with acrylic acid and methacrylic acid showed pH responsive behavior and while acrylamide based nexus exhibited pH independent style in swelling and drug release. However, among all the formulations, maximum swelling ratio (25.86) and optimal prolonged drug release (82.92%) was observed for GG-co-AA (M2) polymeric network at intestinal pH 7.4. The results indicated that GG-co-AA polymeric network could be an impending pH-sensitive drug delivery system for Losartan potassium. (M2) designated as formulation code with varying acrylic acid contents.
Subject(s)
Angiotensin Receptor Antagonists , Losartan , Angiotensin-Converting Enzyme Inhibitors , Polymers , AcrylamidesABSTRACT
Leishmaniasis is affirmed as a category one disease (most emerging and unmanageable) by the World Health Organization (WHO), affecting 98 countries with an annual global incidence of ~1.2 million cases. Options for chemotherapeutic treatment are limited due to drug resistance and cytotoxicity. Thus, the search for new chemical compounds is instantly desirable. In this study, we used two compounds, i.e., 10-hydroxy chondrofoline and tafenoquine, for their antileishmanial activity against L. tropica (HTD7). First, the cytotoxicity assay of the test compounds against THP-1 cells was carried out, and these compounds were found safe. Intra-THP-1 amastigote activity (in vitro) was performed, which was then followed by the in vivo activity of 10-hydroxy chondrofoline in the murine cutaneous leishmaniasis (CL) model. A total of three concentrations were used, i.e., 25, 50, and 100 µM, to check the in vitro activity of the test compounds against the amastigotes. 10-hydroxy chondrofoline was found to be the most potent compound in vitro (and thus was selected for in vivo studies) with an LD50 value of 43.80 µM after 48 h incubation, whilst tafenoquine had an LD50 value of 53.57 µM. In vivo activity was conducted by injecting 10-hydroxy chondrofoline in the left hind foot of the infected BALB/c mice, where it caused a statistically significant 58.3% (F = 14.18; p = 0.002) reduction in lesion size (0.70 ± 0.03 mm) when compared with negative control (1.2 ± 0.3 mm).
ABSTRACT
The present study was conducted to fabricate and compare pH-sensitive polymeric networks of Artemisia vulgaris- Methacrylic acid using free radical polymerization conventional method and microwave-assisted method. Potassium persulphate and N' N'- Methylene bisacrylamide were employed as an initiator-crosslinker system. Swelling studies were performed at pH 1.2, 4.5, 6.8 and 7.4. Concentrations of polymer and monomer along with radiation dose were optimized as a function of swelling. Porosity and gel fraction were calculated for all samples. FTIR study confirmed the formation of cross-linked networks. Results of SEM indicated that the microwave irradiated polymeric network had a more porous structure. DSC and XRD study indicated the entrapment of drug inside the polymeric networks in amorphous form. In comparison to the conventional method, the polymeric network prepared by the microwave-assisted method exhibited high swelling ratios, porosity, thermal stability and drug release. These results signify microwave radiations as an effective alternative to the conventional heating method.
Subject(s)
Artemisia , Drug Liberation , Hydrogels/chemistry , Polymers/chemistry , PolysaccharidesABSTRACT
The objective of this study was to fabricate and evaluate a pH sensitive cross-linked polymeric network through the free radical polymerization technique for the model drug, cyclophosphamide, used in the treatment of non-Hodgkin's lymphoma. The Hydrogels were prepared using a polymeric blend of agarose, Pluronic acid, glutaraldehyde, and methacrylic acid. The prepared hydrogels were characterized for drug loading (%), swelling pattern, release behavior, the ingredient's compatibility, structural evaluation, thermal integrity, and toxicity evaluation in rabbits. The new polymer formation was evident from FTIR findings. The percentage loaded into the hydrogels was in the range of 58.65-75.32%. The developed hydrogels showed significant differences in swelling dynamics and drug release behavior in simulated intestinal fluid (SIF) when compared with simulated gastric fluid (SGF). The drug release was persistent and performed in a controlled manner for up to 24 h. A toxicity study was conducted on white albino rabbits. The developed hydrogels did not show any signs of ocular, skin, or oral toxicity; therefore, these hydrogels can be regarded as safe and potential carriers for controlled drug delivery in biomedical applications.
ABSTRACT
The aim of this contemporary work was to formulate a controlled release mucoadhesive nanoparticle formulation for enhancing the oral bioavailability of Ticagrelor (TG), a BCS class IV drug, having low oral bioavailability of about 36%. The nanoparticles can act as efficient carriers for hydrophobic drugs, due to having high surface area and hence can improve their aqueous solubility due to their hydrophilic nature. The nanoparticles (NPs) of TG were formulated using chitosan (CH) as polymer and sodium tripolyphosphate (TPP) as cross-linker, by ionic gelation technique with varying concentrations of polymer with respect to TG and TPP. Characterization of prepared nanoparticles was carried out to assess zeta potential, size, shape, entrapment efficiency (EE) and loading capacity (LC), using zeta sizer, surface morphology and chemical compatibility analysis. Drug release was observed using UV-Spectrophotometer. By increasing concentration of CH the desired size of particles (106.9 nm), zeta potential (22.6 mv) and poly dispersity index (0.364) was achieved. In vitro profiles showed a controlled and prolonged release of TG in both lower pH-1.2 and neutral pH-7.4 mediums, with effective protection of entrapped TG in simulated gastric conditions. X-ray diffraction patterns (XRD) showed the crystalline nature of formed NPs. Hence, this effort showed that hydrophobic drugs can be effectively encapsulated in nanoparticulate systems to enhance their solubility and stability, ultimately improving their bioavailability and effectiveness with better patient compliance by reducing dosing frequencies as well.
ABSTRACT
BACKGROUND: Chronic wound healing is a major challenge for the health care system around the globe. The current study was conducted to develop and characterize chemically cross-linked polyethylene glycol-co-poly (AMPS) hydrogel membranes to enhance the wound healing efficiency of antibiotic mupirocin (MP). METHODS: Free radical polymerization technique was used to develop hydrogel membranes. In an aqueous medium, polymer PEG-4000 was cross-linked with the monomer 2-acrylamido-2-methylpropane sulfonic acid (AMPS) in the presence of initiators ammonium peroxide sulfate (APS) and sodium hydrogen sulfite (SHS). N, N-Methylene-bis-acrylamide (MBA) was used as a cross-linker in preparing hydrogel membranes. Developed membranes were spherical, transparent, and had elasticity. FTIR, TGA/DSC, and SEM were used to characterize the polymeric system. Swelling behavior, drug loading, and release pattern at pH of 5.5 and 7.4, irritation study, ex vivo drug permeation, and deposition study were also evaluated. RESULTS: Formed membranes were spherical, transparent, and had elasticity. The formation of a stable polymeric network was confirmed by structural and thermal analysis. Evaluation of the drug permeability in the skin showed good permeation and retention capabilities. No irritancy to the skin was observed. CONCLUSION: Based on the results obtained, the present study concluded that the formulated stable network might be an ideal network for the delivery of mupirocin in skin infections.
Subject(s)
Hydrogels , Mupirocin , Delayed-Action Preparations/chemistry , Hydrogels/chemistry , Polyethylene Glycols , Polymers/chemistry , Wound HealingABSTRACT
The aim of this study was to investigate the potential of Linum usitatissimum mucilage, a natural polymer, in developing a sustained release hydrogel for orally delivered drugs that require frequent dosing. For this purpose, nicorandil (a model drug)-loaded hydrogels with various feed ratios of Linum usitatissimum mucilage, acrylamide (monomer) and methylene bis-acrylamide (crosslinker) were prepared. The newly synthesized hydrogel formulations were probed fundamentally with respect to swelling behaviour, solvent penetration, and the release of the drug from the hydrogels. Later, the selected formulations were further characterized by Fourier-transform infrared spectroscopy, thermal analysis, X-ray diffraction analysis, and scanning electron microscopy. The swelling coefficient demonstrated a linear relation with the polymer ratio; however, an inverse behaviour in the case of monomer and crosslinker was observed. The drug release studies, performed at pH 1.2 and 4.5 and considering the dynamic environment of GIT, demonstrated that all formulations followed the Korsmeyer-Peppas model, displaying a slow drug release via diffusion and polymer erosion. FTIR analysis confirmed the successful grafting of acrylamide on linseed mucilage. Furthermore, scanning electron microscopy revealed a clear surface morphology with folds and pinholes in the hydrogel. Therefore, based upon the in-vitro outcomes, it can be concluded that a promising sustained release hydrogel can be prepared from natural polymer, Linum usitatissimum mucilage, offering many-fold benefits over the conventional synthetic polymers for oral delivery of drugs.
ABSTRACT
[This corrects the article DOI: 10.3389/fchem.2020.00050.].
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Natural mucilages are auspicious biodegradable polymeric materials. The aim of the present research work was to elucidate the characteristics of quince mucilage-based polymeric network for sustained delivery of metprolol tartrate and its toxicity evaluation. Mucilage was extracted by hot water extraction, and characterization of quince mucilage was accomplished by using Fourier transform infrared (FTIR) spectroscopy. Different batches of quince mucilage polymeric network were prepared by free radical polymerization by utilizing varying ratios of quince mucilage, acrylamide and crosslinker. Degree of swelling depends on concentration of mucilage, monomer and also on crosslinking density of polymeric network. FTIR illustrates proficient grafting, and morphological (scanning electron microscopy) analysis signified porous design. Hence, quince mucilage-based design was encouraging for sustained delivery of metprolol tartrate and acute toxicity evaluation proved that mucilage-based network was safe for oral drug delivery system.
ABSTRACT
Routinely used anti-inflammatory drugs are associated with off-target effects such as cyclooxygenase (COX)-1 inhibition and gastric ulcers. The aim of this study is to examine the anti-inflammatory potential and gastroprotective effects of synthetic amino acid derivatives of 2-mercaptobenzimidazole (MBAA1, MBAA2, MBAA3, MBAA4 and MBAA5). The results showed that compound MBAA5 possess a potential anti-inflammatory action by inhibition of 15-LOX and COX-2. MBAA5 also attenuated the pro-inflammatory cytokines and mediators (TNF-α, IL-1ß and COX-2) in rat hind paw in carrageenan-induced inflammatory model of rat. 2-mercaptobenzimidazole derivative, MBAA5 also inhibited gastric H+/K+ ATPase and demonstrated a better selectivity index for COX-2 (SI 27.17) in comparison to celecoxib (SI 41.43). Molecular docking studies predicted the binding interactions of the synthesized compounds with retrieved target proteins of H+/K+ ATPase, COX-1, COX-2, and 15-LOX. The results of in silico and molecular docking analysis of amino acid derivatives of 2-mercaptobenzimidazoles further explained their pharmacological activities. Moreover, these compounds presented better antimicrobial activity against three clinical isolates of Helicobacter pylori. Together, our findings suggested that these synthetic 2-mercaptobenzimidazole derivatives are safer therapeutic candidates for inflammation.
Subject(s)
Amino Acids/pharmacology , Arachidonate 15-Lipoxygenase/drug effects , Benzimidazoles/pharmacology , Cyclooxygenase 2/drug effects , Cytokines/drug effects , H(+)-K(+)-Exchanging ATPase/drug effects , Amino Acids/chemistry , Animals , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Arachidonate 15-Lipoxygenase/metabolism , Benzimidazoles/chemistry , Carrageenan , Computer Simulation , Cyclooxygenase 1/drug effects , Cyclooxygenase 1/metabolism , Cyclooxygenase 2/metabolism , Cyclooxygenase 2 Inhibitors/pharmacology , Cytokines/metabolism , H(+)-K(+)-Exchanging ATPase/metabolism , Helicobacter pylori/drug effects , Inflammation/metabolism , Interleukin-1beta/drug effects , Interleukin-1beta/metabolism , Lipoxygenase Inhibitors/pharmacology , Molecular Docking Simulation , Rats , Stomach Ulcer/chemically induced , Tumor Necrosis Factor-alpha/drug effects , Tumor Necrosis Factor-alpha/metabolismABSTRACT
In this work, series of pH-responsive hydrogels (FMA1-FMA9) were synthesized, characterized, and evaluated as potential carrier for oral delivery of an antiviral drug, acyclovir (ACV). Different proportions of ß-cyclodextrin (ß-CD), chitosan (CS), methacrylic acid (MAA) and N' N'-methylenebis-acrylamide (MBA) were used to fabricate hydrogels via free radical polymerization technique. Fourier transform infrared spectroscopy confirmed fabrication of new polymeric network, with successful incorporation of ACV. Scanning electron microscopy (SEM) indicated presence of slightly porous structure. Thermal analysis indicated enhanced thermal stability of polymeric network. Swelling studies were carried out at 37 °C in simulated gastric and intestinal fluids. The drug release data was found best fit to zero-order kinetics. The preliminary investigation of developed hydrogels showed a pH-dependent swelling behavior and drug release pattern. Acute oral toxicity study indicated no significant changes in behavioral, clinical, or histopathological parameters of Wistar rats. Pharmacokinetic study indicated that developed hydrogels caused a significant increase in oral bioavailability of ACV in rabbit plasma as compared to oral suspension when both were administered at a single oral dose of 20 mg kg-1 bodyweight. Hence, developed hydrogel formulation could be used as potential candidate for controlled drug delivery of an antiviral drug acyclovir.
Subject(s)
Acyclovir/pharmacokinetics , Antiviral Agents/pharmacokinetics , Chitosan/chemistry , Hydrogels/chemistry , beta-Cyclodextrins/chemistry , Acrylamides/chemistry , Acyclovir/administration & dosage , Acyclovir/adverse effects , Animals , Antiviral Agents/administration & dosage , Antiviral Agents/adverse effects , Area Under Curve , Chemistry, Pharmaceutical , Delayed-Action Preparations , Dose-Response Relationship, Drug , Drug Delivery Systems , Drug Liberation , Female , Hydrogen-Ion Concentration , Metabolic Clearance Rate , Methacrylates/chemistry , Rabbits , Rats , Rats, Wistar , Surface PropertiesABSTRACT
In the present study, we synthesized silver (Ag) nanoparticles using aqueous extracts of clove (Syzygium aromaticum) (SAE). This synthesis of green silver nanoparticles (AgNP) was a novel and effectual tool against the Newcastle Viral Disease (NDV). Syzygium aromaticum extract was used as reducing and stabilizing agent for synthesis of silver nanoparticles. AgNP were characterized using diversity of biophysical methods inclusive of Fourier transform infrared spectroscopy (FTIR), UV-VIS spectroscopy and Transmission electron microscopy (TEM) for morphology and size. Furthermore, XRD analysis confirmed the crystalline nature of the particles. In current investigations, the antiviral activity of clove buds silver nanoparticles was inspected in-vitro and in-ovo. Embryonated chicken eggs were used to perform the cytotoxicity assay of the clove extract silver nanoparticles (CESN). CESN showed in vitro antiviral activity against NDV in embryonated eggs.
Subject(s)
Antiviral Agents/pharmacology , Metal Nanoparticles/administration & dosage , Plant Extracts/pharmacology , Silver/pharmacology , Syzygium/chemistry , Animals , Chickens , Green Chemistry Technology/methods , Newcastle Disease/drug therapy , Newcastle disease virus/drug effects , Spectroscopy, Fourier Transform Infrared/methods , Water/chemistryABSTRACT
Benzimidazole is an important pharmacophore for clinically active drugs against inflammation and treatment of pain, however, it is associated with gastrointestinal side effects. Here we synthesized benzimidazole based agents with significant analgesic/anti-inflammatory potential but with less gastrointestinal adverse effects. In this study, we synthesized novel, orally bioavailable 2-mercaptobenzimidazole amino acid conjugates (4a-4o) and screened them for analgesic, anti-inflammatory and gastro-protective effects. The synthesized 2-mercaptbenzimidazole derivatives were characterized for their structure using FTIR, 1 H NMR and 13 C NMR spectroscopic techniques. The 2-mercaptobenzimidazole amino acid conjugates have found to possess potent analgesic, anti-inflammatory and gastroprotective activities, particularly with compound 4j and 4k. Most of the compounds exhibited remarkable anti-ulcer and antisecretory effects. Molecular docking studies were carried out to study the binding affinities and interactions of the synthesized compounds with target proteins COX-2 (PDB ID: 3LN1) and H+ /K+ -ATPase (PDB ID: 5Y0B). Our results support the clinical promise of these newly synthesized 2-mercaptobezimidazol conjugates as a component of therapeutic strategies for inflammation and analgesia, for which the gastric side effects are always a major limitation.
ABSTRACT
This study investigated the use of pure polymer chitosan (CS), xanthan gum (XG), monomer 2-acrylamido-2-methylpropane sulfonic acid (AMPS) and initiator potassium persulfate (KPS) as drug carrier system crosslinked through N' N'-methylene bis-acrylamide (MBA) for controlled drug delivery of acyclovir (ACV). ACV is highly effective and selective antiviral drugs used for prophylaxis and treatment against herpes simplex viruses (HSV) infections. Present oral marketed formulations are associated with number of side effects and shortcomings which hampered its clinical effectiveness. Hydrogels (FCX1-FCX9) composed of CS, XG, AMPS, MBA, and KPS were prepared by free radical polymerization technique and characterized through FTIR, PXRD, thermal analysis and SEM. Swelling dynamics and drug release behavior was also investigated. FTIR studies confirmed that ACV was successfully encapsulated into hydrogel polymeric network. SEM revealed porous structure whereas thermal analysis showed enhanced thermal stability of polymeric network. PXRD indicated amorphous dispersion of ACV during preparation process. Swelling dynamics and ACV release behavior from developed hydrogels was dependent on pH of the medium and concentration of pure reactants used. Korsmeyer-Peppas model was best fit to regression coefficient. The present work demonstrated a potential for developing a pH sensitive hydrogel for an antiviral drug ACV by using pure polymers CS, XG, and monomer AMPS.