scholarly journals Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies

Materials ◽  
2021 ◽  
Vol 14 (21) ◽  
pp. 6291
Author(s):  
Mansi Bhanderi ◽  
Jigar Shah ◽  
Bapi Gorain ◽  
Anroop B. Nair ◽  
Shery Jacob ◽  
...  

Rivastigmine, a reversible cholinesterase inhibitor, is frequently indicated in the management of demented conditions associated with Alzheimer disease. The major hurdle of delivering this drug through the oral route is its poor bioavailability, which prompted the development of novel delivery approaches for improved efficacy. Due to numerous beneficial properties associated with nanocarriers in the drug delivery system, rivastigmine nanoparticles were fabricated to be administer through the intranasal route. During the development of the nanoparticles, preliminary optimization of processing and formulation parameters was done by the design of an experimental approach. The drug–polymer ratio, stirrer speed, and crosslinking time were fixed as independent variables, to analyze the effect on the entrapment efficiency (% EE) and in vitro drug release of the drug. The formulation (D8) obtained from 23 full factorial designs was further coated using Eudragit EPO to extend the release pattern of the entrapped drug. Furthermore, the 1:1 ratio of core to polymer depicted spherical particle size of ~175 nm, % EE of 64.83%, 97.59% cumulative drug release, and higher flux (40.39 ± 3.52 µg·h/cm2). Finally, the intranasal ciliotoxicity study on sheep nasal mucosa revealed that the exposure of developed nanoparticles was similar to the negative control group, while destruction of normal architecture was noticed in the positive control test group. Overall, from the in vitro results it could be summarized that the optimization of nanoparticles’ formulation of rivastigmine for intranasal application would be retained at the application site for a prolonged duration to release the entrapped drug without producing any local toxicity at the mucosal region.

2018 ◽  
Vol 11 (13) ◽  
pp. 225
Author(s):  
Sulaeman A ◽  
Patonah Patonah ◽  
Patonah Patonah ◽  
Negara Gg ◽  
Negara Gg

  Objective: The effect of Zingiber ottensii Val. rhizome and Sauropus androgynus L. Merr leaves extract combination was investigated using histologic profile of adipose tissues in obese male rats induced by high-fat and carbohydrate diets.Methods: This was a preventive study, conducted for 42 days by simultaneous administration of diets and extracts administration. The subjects were divided into 8 groups. All groups except negative control group were fed with high-fat and carbohydrate diets. Orlistat, metformin, and curcumin were used as contrast.Result: The phytochemical screening of Z. ottensii Val. rhizome extract showed the presence of flavonoids, saponins, and triterpenoids, meanwhile S. androgynus L. Merr leaves extract presented flavonoids, tannins, saponins, steroids, and triterpenoids. The results showed tissues histological differences in all test group compared with positive control. The most effective combination dose for bangle and katuk leaves extract in protecting adipose tissue was 100 mg/Kg:100 mg/Kg body weight.Conclusion: The combination of black bangle and katuk leaves extract showed a protective role, demonstrated by adipose tissues histologic profile.


2020 ◽  
Vol 6 (3) ◽  
pp. 157
Author(s):  
Adinningtyas Intansari ◽  
Al Munawir ◽  
Laksmi Indreswari

Physalia utriculus is one of the invertebrate marine biota that is often found in Indonesia. Some symptoms of venoming due to jellyfish stings cause pain, itching, and hemolysis. In Indonesia, 13 cases of jellyfish stings were reported in 2005-2009 with three people dying in Java, Bali, and Bangka. Cocoa beans (Theobroma cacao L.) contain fat, carbohydrates, proteins, and polyphenol compounds that are useful as antioxidants. Polyphenols in the form of epicathechins, catechins, and procyanidins serve to provide protection to hemolysis. The purpose of this study was to determine the potential of ethanol extract of cacao (Theobroma cacao L.) in inhibiting the damage of erythrocyte induced by Physalia utriculus in vitro. This study used 28 samples of erythrocytes divided into seven groups, namely the normal control group, negative controls, and treatment with cocoa ethanol extract 0.2%, 0.1%, 0.04%, and 0.02%. Each subsequent group induced venom Physalia utriculus. The results showed that the average speed of erythrocyte lysis in the treatment group by giving cocoa ethanol extract 0.2%, 0.1%, 0.04%, and 0.02% respectively (seconds ± standard deviation) was 858,25 ± 94,44; 1.000,5 ± 159,93; 678,5 ± 19,71; and 1.006 ± 159,50. The mean speed of erythrocyte lysis in the negative control group was 1,025 ± 164.63 and the positive control group with the administration of N-Acetylcystein can last up to one hour after administration of venoms. Test for normality and homogeneity shows that data is normally distributed and homogeneous. One Way Annova analysis shows the significance value of p <0.05, then a post hoc analysis test was performed with the Bonferoni method to find out the differences in significance in each group. In this study it can be concluded that the administration of cocoa ethanol extract has no potential to inhibit erythrocyte damage that has been venomed by Physalia utriculus in vitro. Keywords: Physalia utriculus, cacao, erythrocyte damage


2020 ◽  
Author(s):  
Manisha Nepal ◽  
Snigdha Shubham ◽  
Rupam Tripathi ◽  
Jwolan Khadka ◽  
Deepa Kunwar ◽  
...  

Abstract Background The present study compares the apical microleakage of three different root-end filling materials in which the retrograde cavity is prepared by two different burs. Methods Eighty extracted single rooted maxillary and mandibular premolars were taken. Root canal treatment was completed. Apical 3 mm of all the teeth were resected with diamond disk. The tooth were divided into four groups with two subgroups for each group containing 10 tooth (N= 10) as: Group IA (Negative Control and IB (Positive Control); Group IIA and IIB: Prepared with round carbide bur and round diamond bur respectively, filled with GIC; Group IIIA and IIIB: Prepared with round carbide bur and round diamond bur respectively, filled with MTA; Group IVA and IVB: Prepared with round carbide bur and round diamond bur, filled with Biodentine. After applying two coats of nail varnish leaving apical 3 mm (except for negative control group) all teeth were immersed in 2% methylene blue for 3 days and again in 65% nitric acid for next 3 days for extraction of dye. The obtained solution was then transferred to eppendorf tube and centrifuged in microcentrifuges at 14,000 revolution per minutes (RPM) for 5 minutes. Optical density or absorbance of the supernatant solution was measured with UV spectrophotometer at 550 nm. Results The absorbance of the supernatant solution after dye extraction is decreasing in the order of positive control> GIC> MTA> Biodentine> negative control group. The significant difference was observed between GIC and MTA (p=0.0001) and GIC and Biodentine (p=0.0001) with two different burs but statistically non-significant difference was observed between MTA and Biodentine with Carbide bur (p=0.127) and Diamond bur (p=0.496) respectively. Conclusions Within the limitations of the present study, it can be concluded that Biodentine and MTA showed less microleakage as compared to GIC. There is no significant difference between mean microleakage of MTA and Biodentine. However, the mean OD of the Biodentine was least of all evaluated materials. Preparation of the root-end using round carbide bur as well as round diamond burs showed comparable microleakage for all three filling materials.


2020 ◽  
Vol 54 (4) ◽  
pp. 336-342
Author(s):  
Philipp Körner ◽  
Jana A Schleich ◽  
Daniel B. Wiedemeier ◽  
Thomas Attin ◽  
Florian J. Wegehaupt

<b><i>Objectives:</i></b> This in vitro study aimed to evaluate and compare the effect of two different bioactive glasses, a hydroxyapatite-containing, fluoride-free toothpaste (HTP) and a fluoride toothpaste (FTP) on the remineralization behavior of initial caries lesions. <b><i>Materials and Methods:</i></b> A total of 100 bovine enamel samples were randomly allocated to five groups of 20 samples each: NC = negative control group (artificial saliva); HTP = HTP group (Karex); FTP = FTP group (Elmex caries protection, 1,400 ppm); FTP + BG<sub>nano</sub> = FTP followed by Actimins bioactive glass; FTP + BG<sub>amorph</sub> = FTP followed by Schott bioactive glass. Radiographic documentation (advanced transversal microradiography; aTMR) was applied before and after all samples were exposed to a demineralizing gel for 10 days. Over a period of 28 days, samples were covered twice a day (every 12 h) with a toothpaste slurry of the respective test group or with artificial saliva in NC for 60 s and brushed with 15 brushing strokes. Samples in FTP + BG<sub>nano</sub> and FTP + BG<sub>amorph</sub> were additionally treated with the respective bioactive glass slurry for 30 s after brushing with the FTP. In the meantime, all samples were stored in artificial saliva. After 28 days, the structure of all samples was assessed again using aTMR and compared to the values measured after demineralization. The statistical evaluation of the integrated mineral loss was performed using Kruskal-Wallis test followed by a post hoc Conover test. <b><i>Results:</i></b> The FTP revealed the significantly highest increase of mineral content while the HTP showed the significantly lowest remineralization. Compared to artificial saliva, the use of the HTP or the combined application of FTP followed by bioactive glasses (FTP + BG<sub>nano</sub> and FTP + BG<sub>amorph</sub>) showed no significant remineralization. <b><i>Conclusion:</i></b> Under remineralizing in vitro conditions, brushing with 1,400 ppm FTP induced significantly more remineralization compared to storage in artificial saliva. The additional administration of both bioactive glasses as well as the substitutional brushing with an HTP resulted in significantly less remineralization compared to brushing with 1,400 ppm FTP.


2016 ◽  
Vol 50 (3) ◽  
pp. 337-345 ◽  
Author(s):  
N.I.P. Pini ◽  
D.A.N.L. Lima ◽  
J.R. Lovadino ◽  
C. Ganss ◽  
N. Schlueter

The present study evaluated the effect of chitosans with different viscosities, dissolved in an AmF/SnCl2 solution, against erosion or erosion/abrasion. A total of 192 specimens were assigned to 2 × 6 groups (n = 16 specimens each): negative control, 4 chitosan solutions (groups Ch50, Ch500, Ch1000, and Ch2000, with viscosity of 50, 500, 1,000, or 2,000 mPas, respectively, 0.5% chitosan, 500 ppm F-, 800 ppm Sn2+, pH 4.4), and positive control (500 ppm F-, 800 ppm Sn2+, pH 4.3). One half of the groups was demineralized (experiment 1, E1; 10 days, 6 × 2 min/day, 0.5% citric acid, pH 2.8) and exposed to solutions (2 × 2 min/day); the other half was additionally brushed (15 s, 200 g) with non-fluoridated toothpaste before solution immersion (experiment 2, E2). Treatment effects were investigated by profilometry, energy-dispersive X-ray spectroscopy and scanning electron microscopy (SEM). In E1, all the chitosan-containing solutions reduced enamel loss by 77-80%, to the same extent as the positive control, except for Ch2000 (p ≤ 0.05), which completely inhibited tissue loss by the formation of precipitates. In E2, Ch50 and Ch500 showed best performance, with approximately 60% reduction of tissue loss compared to the negative control group (p ≤ 0.05 compared to other groups). SEM analysis showed differences between negative control and the other groups but only minor differences amongst the groups treated with active agents. In both E1 and E2, treatment with active agents resulted in surface enrichment of carbon and tin compared to negative control (p ≤ 0.001); brushing removed parts of carbon and tin (p ≤ 0.001). Chitosan shows different properties under erosive and erosive/abrasive conditions. Under erosive conditions high viscosity might be helpful, whereas lower viscosity seems to be more effective in cases of chemo-mechanical challenges.


Author(s):  
Ni Nyoman Yuliani ◽  
Jefrin Sambara ◽  
Maria Hilaria ◽  
Harlinda Harlinda

Indonesia has  biodiversity potential to be developed as medicinal plants, such as basil leaves (Ocimum sanctum L.). Basil was reported to have a very high antioxidant activity in vitro. The aim of this study was to determine the effect of basil leaves (Ocimum sanctum L.) infusion to liver based Aspartate Aminotransferase (AST) and Alanine Aminotransferase (ALT) value in each dose. 18 rats were divided into 6 groups.,  control group,  negative control group treated with CMC Na 0.5%,  positive control group treated with Curcuma 3.6 mg / 200gBB, groups of 4-6 consecutive given a 80 mg  dose infusion basil / 200 gBB, 160 mg / 200 gBB, 320 mg / 200 gBB for 8 consecutive days, on the day of the 4th and 8th all treatment groups induced by toxic doses of paracetamol (500 mg / 200 gBB) except the normal control group 1, The research data in the form of enzyme activity of AST and ALT were analyzed using parametric and nonparametric ANOVA, and Friedman test with the level of trust  then followed by SNK test and Bnj test. The statistical test result with a 95% of level of trust that shown basil infuse with a dose of 80mg / 200gBB, 160mg / 200gBB, 320mg / 200gBB have hepatoprotective effects in rats induced by paracetamol 500mg / 200gBB. Based on the result of changes in average levels of AST on the fourth day and the eighth day of the three treatment infusion, infusion at a dose of 160 mg / 200gBB most effectively reduce average levels of AST and a group that has the average AST closest to the control group is positive, but infusion at a dose of 320mg / 200gBB the group that has the closest average ALT positive control group.Keywords : hepatoprotective, Ocimum sanctum L, Paracetamol


2011 ◽  
Vol 35 (4) ◽  
pp. 393-396 ◽  
Author(s):  
P Subramaniam ◽  
U Eswara ◽  
KL Girish Babu ◽  
B Vardhan

Objective: To assess the efficacy of Oral Rehydration Salt-Liquid (ORS-L) in the maintenance of the viability of Periodontal ligament cells (PDL). Materials and Method: Twenty freshly extracted teeth were used for this study. They were then randomly divided into 3 groups: Positive control group - 5 teeth which were immediately subjected to collagenase assay, without immersing in ORS-L; Negative control group - 5 teeth with an extra oral dry time of 24 hours, followed by subjecting to collagense assay without immersing in ORS-L and Test group (ORS-L) - 10 teeth with an extra oral dry period of 30 minutes, followed by immersion in ORS-L for a period of 45 minutes and then subjected to collagenase assay. The mean number of viable PDL cells were counted on a hemocytometer under 20X magnification. Results: The mean number of viable PDL cells was highest in the positive control group. In comparison to the negative control group, the test group showed a higher number of viable PDL cells. Conclusion: The study found that ORS-L was an effective solution in maintaining the viability of PDL cells.


2011 ◽  
Vol 55 (6) ◽  
pp. 2597-2600 ◽  
Author(s):  
Nicolas Veziris ◽  
Chantal Truffot ◽  
Jean-Luc Mainardi ◽  
Vincent Jarlier

ABSTRACTAlthough beta-lactam antibiotics are not considered as antituberculous drugs, it has been recently shown that the combination of carbapenems and clavulanate is bactericidalin vitro. We evaluated in a murine model of tuberculosis the activity of carbapenems alone and combined with clavulanate againstMycobacterium tuberculosis. Swiss mice infected intravenously with 3 × 105M. tuberculosisH37Rv were treated for 4 weeks with clavulanate alone or imipenem, meropenem, and ertapenem alone or combined with clavulanate, whereas a positive control group was treated with isoniazid, and a negative control group was held without treatment. The combination of imipenem or meropenem plus clavulanate significantly improved survival. Among groups of mice with 100% survival, only isoniazid reduced lung CFU counts; the carbapenem-clavulanate combinations did not prevent bacterial growth. Although less active than isoniazid, the combinations of imipenem or meropenem plus clavulanate improved the survival of mice infected withM. tuberculosisand should be further evaluated.


2020 ◽  
Author(s):  
Manisha Nepal ◽  
Snigdha Shubham ◽  
Rupam Tripathi ◽  
Jwolan Khadka ◽  
Deepa Kunwar ◽  
...  

Abstract Background The present study compares the apical microleakage of three different root-end filling materials in which the retrograde cavity is prepared by two different burs.Methods Eighty extracted single rooted maxillary and mandibular premolars were taken. Root canal treatment was completed. Apical 3 mm of all the teeth were resected with diamond disk. The tooth were divided into four groups with two subgroups for each group containing 10 tooth (N= 10) as: Group IA (Negative Control and IB (Positive Control); Group IIA and IIB: Prepared with round carbide bur and round diamond bur respectively, filled with GIC; Group IIIA and IIIB: Prepared with round carbide bur and round diamond bur respectively, filled with MTA; Group IVA and IVB: Prepared with round carbide bur and round diamond bur, filled with Biodentine. After applying two coats of nail varnish leaving apical 3 mm (except for negative control group) all teeth were immersed in 2% methylene blue for 3 days and again in 65% nitric acid for next 3 days for extraction of dye. The obtained solution was then transferred to eppendorf tube and centrifuged in microcentrifuges at 14,000 revolution per minutes (RPM) for 5 minutes. Optical density or absorbance of the supernatant solution was measured with UV spectrophotometer at 550 nm.esults The absorbance of the supernatant solution after dye extraction is decreasing in the order of positive control> GIC> MTA> Biodentine> negative control group. The significant difference was observed between GIC and MTA (p=0.0001) and GIC and Biodentine (p=0.0001) with two different burs but statistically non-significant difference was observed between MTA and Biodentine with Carbide bur (p=0.127) and Diamond bur (p=0.496) respectively.Conclusions Within the limitations of the present study, it can be concluded that Biodentine and MTA showed less microleakage as compared to GIC. There is no significant difference between mean microleakage of MTA and Biodentine. However, the mean OD of the Biodentine was least of all evaluated materials. Preparation of the root-end using round carbide bur as well as round diamond burs showed comparable microleakage for all three filling materials.


Author(s):  
Thalles D’avila Pires Dutra Dantas ◽  
Francisco Marlon Carneiro Feijó ◽  
Nilza Dutra Alves ◽  
Gardênia Silvana De Oliveira Rodrigues ◽  
Caio Sérgio dos Santos ◽  
...  

This survey evaluated mombin leaves (Spondias mombin L.) decoction efficiency as an antiseptic during post-surgery period on cats submitted to orchiectomy and ovariosalpingohisterectomy. For this purpose, 45 castrated mongrels cats were divided into three groups, the first group as a positive control using 0.5% chlorhexidine-alcohol solution, the second a negative control group using sterile distilled water and, finally, the test group using mombin leaves decocted with a concentration of 100 mg/mL. All animals, independent of age and sex, had visibly healed in most cases in a similar time. Animals treated with mombin leaves decoction presented a significant reduction of bacterial growth. In addition, the animals treated in the test group had better surgical wound healing. All isolated bacterial strains presented inhibition halo for chlorhexidine and for Spondias mombin L. Thus, the decoction of Spondias mombin L. leaves proved antiseptic efficacy in the surgical wounds of cats submitted to orchiectomy and ovariosalpingohisterectomy.


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