In vitro ovicidal activity of poly lactic acid curcumin-nisin co-entrapped nanoparticle against Fasciola spp. eggs and its reproductive toxicity

2018 ◽  
Vol 29 (1) ◽  
pp. 73-79 ◽  
Author(s):  
Oyetunde Oyeyemi ◽  
Odunayo Adegbeyeni ◽  
Ifeoluwa Oyeyemi ◽  
Jairam Meena ◽  
Amulya Panda
Keyword(s):  
Reproductive Toxicity ◽  
Entrapment Efficiency ◽  
Negative Control ◽  
Poly Lactic Acid ◽  
Sperm Cells ◽  
Ovicidal Activity ◽  
Egg Hatching ◽  
The Mean

AbstractBackground:Curcumin and nisin have been widely reported for their antibacterial and anticancer potency. However, their therapeutic applications are hampered by several factors, which necessitate their development into nanosize ranges for improved delivery and activities. Their incorporation into a single nanosynthesized form may suggest desirable efficacy on parasites. The aim of the study was to assess the ovicidal activity of the curcumin-nisin polylactic acid (PLA) entrapped nanoparticle on theFasciolaeggs and its reproductive toxicity.Methods:The nanoparticle was formulated by double emulsion method. The eggs of the adultFasciolaspp. were exposed to different concentrations (0.3125–5 mg/mL) of the nanoparticle to monitor hatchability. Mice were exposed to 0.5 mL of the formulated drug at varying concentrations (10–20 mg/kg) and then sacrificed for sperm morphology assay.Results:The mean particle size, polydispersity index, and drug entrapment efficiency of the formulated drug were 288.4±24.3 nm, 0.232, and 51.7%, respectively. The highest nanoparticulate concentration (5 mg/mL) showed the least percentage egg hatching (41.7%) compared with the other treatment groups and positive control (albendazole) (45.1%). The aberrations observed in sperm cells were not concentration-dependent and no significant differences were observed in the mean aberrations between the nanoparticulate drug-exposed groups and the negative control (p>0.05).Conclusions:The results confirmed the ovicidal activity of the curcumin-nisin nanoparticulate drug against theFasciolaspecies. The formulation also showed no toxicity to sperm cells. More robust studies on anti-fascioliasis activity of the drug on adultFasciolaspp. andin vivoandin vitrotoxicity studies are recommended.

Controlled Release Characteristics of PLA-Pluronic-PLA Nano-Sized Vesicles In Vitro

2013 ◽  
Vol 785-786 ◽  
pp. 493-497
Author(s):  
Yu Ping Li ◽  
Li Zhen Sun ◽  
Xiang Yuan Xiong ◽  
Zi Ling Li ◽  
Ting Kang Xing ◽  
...  
Keyword(s):  
Controlled Release ◽  
Protein Delivery ◽  
Phosphate Buffer Solution ◽  
Entrapment Efficiency ◽  
Poly Lactic Acid ◽  
Oral Insulin ◽  
Buffer Solution ◽  
The Mean ◽  
The Stability

In the present study, controlled release characteristics of new nanosized PLA-Pluronic-PLA block copolymer vesicles comprising of amphiphilic poly (lactic acid) (PLA) and Pluronic block copolymers (PEO-PPO-PEO) have been evaluated as an oral insulin carrier. The mean size of vesicles was 78 nm for PLA-F127-PLA and 165 nm for PLA-P85-PLA copolymer. The mean insulin entrapment efficiency was 59.6% for PLA-P85-PLA and 26.4% for PLA-F127-PLA. The in vitro release characteristics of insulin from vesicles exhibited an initial burst in the range of pH 1.2-7.4 dissolution mediums. The presence of PLA-Pluronic-PLA vesicles improved the stability of insulin in the gastrointestinal fluids than that of the phosphate buffer solution (PBS) of insulin. More importantly, the released insulin from the vesicles maintained their biological activity. The results from this studies demonstrated that biodegradable PLA-Pluronic-PLA can self-assemble with insulin, form insulin-encapsulated vesicles, and is good carrier materials for oral insulin/protein delivery.

scholarly journals Formulation and in-vitro evaluation of a transdermal patch loaded with letrozole

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 997-1005
Author(s):  
Kondapuram Parameshwar ◽  
Suvendu Kumar Sahoo ◽  
Rabinarayan Parhi ◽  
Ravi Kumar V ◽  
Ahad Ahmed kodipad ◽  
...  
Keyword(s):  
Entrapment Efficiency ◽  
Transdermal Patch ◽  
Self Administration ◽  
Skin Targeting ◽  
Attractive Option ◽  
Prime Objective ◽  
The Mean ◽  
Transdermal Route

The prime objective behind this investigation was to plan a Letrozole enclosed adhesive transdermal patch; since the transdermal route is an outright attractive option concerning its route, convenience and safety. Letrozole, a non-steroidal type II aromatase inhibitor, is reported for treating breast tumours and in postmenopausal women. In this study, few factors confined to formulation such as drug-in-adhesive, enhancers and amount of drug-loaded were investigated. The procedure used supposedly involves, the incarnation of the LET in phospholipids exploiting to a spray dryer. FTIR, X-RD, and DSC techniques which are used to evaluate entrapment efficiency were employed to LET spray-dried powder (LT-SDP). The molecule size, polydispersity file, and the EE were allegedly found to be 284.0 nm, 0.247 and 59.08%. On adding LT-SDP to a cream base with peppermint and olive oil as regular infiltration, the optimized formulation showed superior skin targeting in both in vitro and in vivo observations post-study.In vivo bioavailability studies showed just about four-fold increment in the plasma whereas the mean residence time and half-life were reasonably higher as compared to the LET cream in plain. The in vivo results observed remarkable patch concurrence with the plasma fixations anticipated from the in vitro infiltration. As an outpatient convenience, avoidance of gastrointestinal incompatibility provides suitability for self-administration for breast cancer prevention and treatment.

scholarly journals Ovicidal activity of succinic acid isolated from sisal waste (Agave sisalana) against gastrointestinal nematodes of goats

2017 ◽  
Vol 47 (8) ◽  
Author(s):  
Nathália Silva de Souza Santos ◽  
Jener David Gonçalves Santos ◽  
Francianne Oliveira Santos ◽  
Taiane Menezes Serra ◽  
Hélimar Gonçalves de Lima ◽  
...  
Keyword(s):  
Succinic Acid ◽  
Anthelmintic Activity ◽  
Vero Cells ◽  
Gastrointestinal Nematodes ◽  
Significant Inhibition ◽  
Egg Hatching ◽  
The Mean ◽  
Agave Sisalana

ABSTRACT: This study was conducted to evaluate the in vitro anthelmintic activity of the succinic acid (SA) isolated from sisal waste against gastrointestinal nematodes of goats, using the egg hatching and larvae motility assays. In addition, potential cytotoxicity of SA on Vero cell cultures was investigated by means of MTT (3-4,5-dimethylthiazol-2-yl, 2,5diphenyltetrazolium bromide) test. The SA induced a significant inhibition of egg hatching (P<0.05) at all concentrations tested (60 to 250µg mL-1), and the concentrations to inhibit 50% (EC50) and 90% (EC90) values (mean ± standard deviation) were 90.3±2.8 and 130.6±3.5µg mL-1, respectively. The SA has not shown larvicidal activity. The SA was less toxic to the Vero cells, with the mean percentage of cell viability equal to 85±6.2% at the concentration of 130µg mL-1. The results suggested that SA has potential anthelmintic effect; although, more research is needed to confirm its activity in vivo.

scholarly journals Anthelminthic effects of extracts of indigenous browses from mid rift valley of Ethiopia

2021 ◽  
Vol 25 (2) ◽  
pp. 132-143
Author(s):  
Amsalu Sisay ◽  
Tegene Negesse ◽  
Ajebu Nurfeta
Keyword(s):  
Developmental Stages ◽  
Negative Control ◽  
In Vitro Assays ◽  
Inhibition Assay ◽  
Egg Hatching ◽  
Acacia Senegal ◽  
Egg Hatch ◽  
Infective Larvae

This study was conducted to evaluate the potential anthelminthic properties of extracts of leaves of indigenous browses (Acacia seyal, Acacia senegal, Acacia tortilis, Millettia ferruginea, and Vernonia amygadalina) based on three in vitro assays. Acetone extracts of browses at different concentrations (75 to 1200 μg/ml, for egg and larvae and 100mg/ml for an adult) were tested on three developmental stages of Haemonchus contortus (eggs, infective larvae, and adult worms) using egg hatch assay (EHA), larval migration inhibition assay (LMIA) and adult worm motility inhibition assay (AMIA). Significant effects were obtained with all five browses but differences were observed depending on the parasitic stages. The effects of five browse extracts on egg hatching were concentration-dependent, the highest (P<0.05) egg hatch inhibition rate was observed at 1200 μg/ml concentration for all browses. All extracts had a higher effect (P<0.01) than that of the negative control, phosphate buffer saline (PBS). In contrast, no concentration-response relationship was found for infective larvae and adult worms, although more potent effects were observed with the highest concentrations. The LMI rate (70%) induced by Vernonia  amygadalina extract, at a concentration of 300 μg/ml, was the highest (P<0.05) of all other browses, even at higher concentrations. The highest LMI rate (62%) induced by Acacia senegal extract at higher concentration, was lower than that of LMI rate (70%) induced by Vernonia amygadalina, at 300 μg/ml concentration. Vernonia amygadalina was found to be highly and rapidly effective against adult worms inducing the highest mortality rate (90%) as soon as 4 hrs after incubation. Overall, the in vitro results suggest that these five  browses do possess anti-parasitic properties and Vernonia amygadalina showed the most effective anti-parasitic property. These effects remain to be confirmed through in vivo study.

scholarly journals Preparation of Prolonged-Circulating Galangin-Loaded Liposomes and Evaluation of Antitumor Efficacy In Vitro and Pharmacokinetics In Vivo

2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Hui Yao ◽  
Hao Lu ◽  
Jun Zhang ◽  
Xuemei Xue ◽  
Chao Yin ◽  
...  
Keyword(s):  
Thin Film ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Pharmacokinetic Parameters ◽  
Pharmacological Effects ◽  
Pegylated Liposomes ◽  
The Mean ◽  
Antibacterial And Antifungal

Galangin has been reported to have many pharmacological effects including being anti-inflammatory, antibacterial, and antifungal and a suppressor of vitiligo, Alzheimer’s disease, and cancer. The purpose of this research was to characterize and determine the efficacy of the antitumor activity and pharmacokinetics of galangin-loaded PEGylated liposomes compared with free galangin. Galangin-loaded liposomes and galangin-loaded PEGylated liposomes were prepared using thin-film dispersion prior to ultrasonication. The mean particle size of the galangin-loaded PEGylated liposomes was approximately 120 nm, the polydispersity index was 0.212, the zeta potential was -2.24 mV, and the entrapment efficiency was 76.31%. The release of galangin from galangin-loaded PEG-modified liposomes was slowest as gauged by dynamic dialysis in vitro. In the apoptosis experiment, galangin-loaded PEG-modified liposomes demonstrated cytotoxicity to hepatoma cells by apoptosis that was greater than the two other forms of drug carrier. In vivo experiments demonstrated that the half-life of galangin in PEG-modified liposomes was 4 hours in the plasma of rats, significantly longer than that of free galangin. The experimental results suggest that the PEG modification of liposomes effectively increases the solubility of galangin and alters its pharmacokinetic parameters, such that it may be effective in the treatment of liver cancer.

scholarly journals Floating microspheres encapsulating carvedilol for the effective management of hypertension

2019 ◽  
Author(s):  
Sapna Patel ◽  
Naina Dubey ◽  
Asmita Gajbhiye ◽  
Shailendra Patil
Keyword(s):  
Surface Morphology ◽  
Delivery System ◽  
Half Life ◽  
Entrapment Efficiency ◽  
Angle Of Repose ◽  
Prolonged Release ◽  
The Mean ◽  
Scanning Electron

Carvedilol (CVD) is an antihypertensive agent with a short half-life, pH-dependent solubility, and narrow absorption window. The purpose of this research was to prepare a floating-drug delivery-system of carvedilol to increase its half-life. The present study investigates the preparation of carvedilol-floating microspheres, evaluates the floatingdrug delivery-system (FDDS) (by scanning electron microscope), it’s in vitro stability, and in vivo profile. Floating microspheres were prepared by solvent-evaporation (oil-in-water emulsion) technique using hydroxypropyl methylcellulose (HPMC) and ethyl cellulose (EC) as the rate controlling polymers. The surface morphology of the prepared microspheres was characterized by scanning electron microscopy. In this study, the particle size analysis, drug entrapment efficiency, surface morphology, buoyancy percentage, and release studies were performed. The microspheres were found to be spherical and porous. The results showed that the mean/mean (SD) values of tapped density, Carr's compressibility index, angle of repose, percentage yield, in vitro buoyancy, %entrapment efficiency of CVD-loaded floating microspheres were 0.42 (0.012), 12.5 (1.895), 23.5 (1.856), 80.2 %, 79.0 %, and 85.81(1.40), respectively. The developed floating-microsphere of CVD released the drug for 24 h and based on in vivo studies, the drug-loaded floating microspheres help in maintaining the mean (SD) systolic blood pressure within the range of 120 (0.32) to 120 (1.02) mmHg and diastolic pressure within 91 (0.71) to 92 (0.79) mmHg. Thus, floating microsphere of CVD offers a suitable and practical approach for prolonged release of the drug over an extended period, and thus improves the oral bioavailability and efficacy of the drug as well as the patient’s compliance.

Influence of Platelet Membrane Sialic Acid and Platelet-Associated IgG on Ageing and Sequestration of Blood Platelets in Baboons

1993 ◽  
Vol 70 (04) ◽  
pp. 676-680 ◽  
Author(s):  
H F Kotzé ◽  
V van Wyk ◽  
P N Badenhorst ◽  
A du P Heyns ◽  
J P Roodt ◽  
...  
Keyword(s):  
Sialic Acid ◽  
Life Span ◽  
Blood Platelets ◽  
Senescent Cell ◽  
Platelet Membrane ◽  
Antigen Complex ◽  
The Mean ◽  
Aggregation Of Platelets

SummaryPlatelets were isolated from blood of baboons and treated with neuraminidase to remove platelet membrane sialic acid, a process which artificially ages the platelets. The platelets were then labelled with 111In and their mean life span, in vivo distribution and sites of Sequestration were measured. The effect of removal of sialic acid on the attachment of immunoglobulin to platelets were investigated and related to the Sequestration of the platelets by the spleen, liver, and bone marrow. Removal of sialic acid by neuraminidase did not affect the aggregation of platelets by agonists in vitro, nor their sites of Sequestration. The removal of 0.51 (median, range 0.01 to 2.10) nmol sialic acid/108 platelets shortened their life span by 75 h (median, range 0 to 132) h (n = 19, p <0.001), and there was an exponential correlation between the shortening of the mean platelet life span and the amount of sialic acid removed. The increase in platelet-associated IgG was 0.112 (median, range 0.007 to 0.309) fg/platelet (n = 25, p <0.001) after 0.79 (median, range 0.00 to 6.70) nmol sialic acid/108 platelets was removed (p <0.001). There was an exponential correlation between the shortening of mean platelet life span after the removal of sialic acid and the increase in platelet-associated IgG. The results suggest that platelet membrane sialic acid influences ageing of circulating platelets, and that the loss of sialic acid may have exposed a senescent cell antigen that binds IgG on the platelet membrane. The antibody-antigen complex may then provide a signal to the macrophages that the platelet is old, and can be phagocytosed and destroyed.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Mannose Conjugated Starch Nanoparticles for Preferential Targeting of Liver Cancer

2020 ◽  
Vol 17 ◽  
Author(s):  
Akhlesh Kumar Jain ◽  
Hitesh Sahu ◽  
Keerti Mishra ◽  
Suresh Thareja
Keyword(s):  
Side Effects ◽  
Liver Cancer ◽  
Entrapment Efficiency ◽  
Xrd Analysis ◽  
In Vitro Cytotoxicity ◽  
Physical Interaction ◽  
Scanning Calorimetry ◽  
Starch Nanoparticles

Aim: To design D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for site specific delivery. Background: Liver cancer is the third leading cause of death in world and fifth most often diagnosed cancer is the major global threat to public health. Treatment of liver cancer with conventional method bears several side effects, thus to undertake these side effects as a formulation challenge, it is necessary to develop novel target specific drug delivery system for the effective and better localization of drug into the proximity of target with restricting the movement of drug in normal tissues. Objective: To optimize and characterize the developed D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for effective treatment of liver cancer. Materials and methods: 5-FU loaded JFSSNPs were prepared and optimized formulation had higher encapsulation efficiency were conjugated with D-Mannose. These formulations were characterized for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning Calorimetry. Potential of NPs were studied using in vitro cytotoxicity assay, in vivo kinetic studies and bio-distribution studies. Result and discussion: 5-Fluorouracil loaded NPs had particle size between 336 to 802nm with drug entrapment efficiency was between 64.2 to 82.3%. In XRD analysis, 5-FU peak was diminished in the diffractogram, which could be attributed to the successful incorporation of drug in amorphous form. DSC study suggests there was no physical interaction between 5- FU and Polymer. NPs showed sustained in vitro 5-FU release up to 2 hours. In vivo, mannose conjugated NPs prolonged the plasma level of 5-FU and assist selective accumulation of 5-FU in the liver (vs other organs spleen, kidney, lungs and heart) compared to unconjugated one and plain drug. Conclusion: In vivo, bio-distribution and plasma profile studies resulted in significantly higher concentration of 5- Fluorouracil liver suggesting that these carriers are efficient, viable, and targeted carrier of 5-FU treatment of liver cancer.

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