<i>In Vitro</i>and<i>In Vivo</i>Evaluation of Niosomal Formulation for Controlled Delivery of Clarithromycin

Asthana, Gyati Shilakari; Sharma, Parveen; Asthana, Abhay

doi:10.1155/2016/6492953

Cited by 96 publications

(47 citation statements)

References 28 publications

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“…It is clear from the results obtained that the niosomes have shown a minimum drug loss at refrigerated condition and fairly high retention of drug inside the vesicles was observed these results were concordant to Asthana et al (2016) [5]. At this low temperature condition only 2.797 % of drug was lost as compared to storage at 25 °C and 37 °C which led to 4.113 % and 5.125 % drug loss respectively at the end of 35 d results shown in (table 6).…”

Section: Drug Leakage Studysupporting

confidence: 74%

“…It was clearly observed from the results that the mean vesicle size of niosomes containing span 20 were found to be higher as compared to other niosomal formulations containing span 40,60 and 80. The vesicle size of niosomal formulation were obtained in the range of 160.1±69.7 nm to718.7±749.9 nm (given in table 3) The vesicle size of niosomes decreased consistently from span 20 to span 80 and are found in the following order-span 20>span 40>span60>span 80 which was in conformance with Asthana et al (2016) [5].…”

Section: Vesicle Size Zeta Potential and Polydispersity Indexmentioning

confidence: 55%

“…These niosomal dispersion are formed from self-assembly of hydrated synthetic non-ionic surfactant monomers which are capable of entrapping a wide variety of drugs both hydrophilic and hydrophobic, can be delivered by various routes like oral, transdermal, parenteral, occular [3] and have been considered superior to microspheres, nanoparticles, liposomes and other carriers in terms of better entrapment of drugs, better target site specificity and in handling burst effect of drug release [4,5]. Niosomes have also shown advantages as drug carriers, such as being low cost and chemically stable as compared to liposomes [6].…”

Section: Introductionmentioning

confidence: 99%

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In Vitro in Vivo Evaluation of Niosomal Formulation of Famotidine

Khan

Irchhaiya

2020

Int J Pharm Pharm Sci

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Objective: The present study was aimed on formulation and evaluation of famotidine loaded niosomal formulation for in vitro and in vivo pharmacokinetic behaviour. Formulating it as niosomal formulation might be quite advantageous for prolonging the duration of pharmacological action and improved bioavailability. Methods:In the present study niosomal formulations were prepared by using most documented thin film hydration technique by using various grades of surfactants (span 20, 40, 60, 80) in varying ratios with cholesterol, negative charge inducer di cetyl phosphate (DCP) and drug famotidine. Suitable preformulation studies were conducted like identification of drug, excipient and drug compatibility study. The optimized drug loaded niosomes were characterized for size and morphology, polydispersity index, zeta potential, drug entrapment, in vitro release, in vivo study and stability study. Results:The results showed that the vesicles formed were spherical in shape, size ranging between 160.1 nm to 718.7 nm with zeta potential values indicating good stability and formulation containing span 60 (NMS7) showed the highest entrapment efficiency (73.234%). All the formulations showed prolonged release profile for more than 24 h with release kinetics better suited to zero order release pattern. In vivo study conducted on rabbits predicted a fourfold increase in pharmacokinetic parameter (area under curve)AUC and pharmacological action for more than 24 h as compared to free drug famotidine which showed its action only upto 12 h. Conclusion:Thus the famotidine loaded niosomal formulation may be considered as a very promising drug delivery system which could be successfully employed for prolonging the drug release and overcoming the drawbacks of conventional drug delivery systems.

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Section: Drug Leakage Studysupporting

confidence: 74%

Section: Vesicle Size Zeta Potential and Polydispersity Indexmentioning

confidence: 55%

Section: Introductionmentioning

confidence: 99%

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In Vitro in Vivo Evaluation of Niosomal Formulation of Famotidine

Khan

Irchhaiya

2020

Int J Pharm Pharm Sci

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“…It is worth noting that the physical stability was performed only at refrigerator temperature, as we found that storing the niosomes at room temperature was proven to negatively affect their stability, due to lowered hydrophobic part rigidity at higher temperature [52].…”

Section: Stability Studiesmentioning

confidence: 98%

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

et al. 2020

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Flavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass effect, poor intestinal absorption and, hence, low systemic bioavailability. A variety of delivery systems have been developed to circumvent these drawbacks, and among them, in this work niosomes have been selected to encapsulate the hepatoprotective natural flavonoid quercetin. The aim of this study was to prepare nanosized quercetin-loaded niosomes, formulated with different monolaurate sugar esters (i.e., sorbitan C12; glucose C12; trehalose C12; sucrose C12) that act as non-ionic surfactants and with cholesterol as stabilizer (1:1 and 2:1 ratio). Niosomes were characterized under the physicochemical, thermal and morphological points of view. Moreover, after the analyses of the in vitro biocompatibility and the drug-release profile, the hepatoprotective activity of the selected niosomes was evaluated in vivo, using the carbon tetrachloride (CCl 4 )-induced hepatotoxicity in rats. Furthermore, the levels of glutathione and glutathione peroxidase (GSH and GPX) were measured. Based on results, the best formulation selected was glucose laurate/cholesterol at molar ratio of 1:1, presenting spherical shape and a particle size (PS) of 161 ± 4.6 nm, with a drug encapsulation efficiency (EE%) as high as 83.6 ± 3.7% and sustained quercetin release. These niosomes showed higher hepatoprotective effect compared to free quercetin in vivo, measuring serum biomarker enzymes (i.e., alanine and aspartate transaminases (ALT and AST)) and serum biochemical parameters (i.e., alkaline phosphatase (ALP) and total proteins), while following the histopathological investigation. This study confirms the ability of quercetin loaded niosomes to reverse CCl 4 intoxication and to carry out an antioxidant effect.Pharmaceutics 2020, 12, 143 2 of 18 and anticancer activities [1][2][3]. These intrinsic properties, together with their biocompatibility and remarkable antioxidant activity, have attracted researchers' attention to explore potential therapeutic applications [4,5].Quercetin (3, 30, 4, 5, 7-pentahydroxyflavone) is probably the most studied bioflavonoid, belonging to the family of flavonols; its therapeutic applications include hepatoprotection [6], prevention of neural cell apoptosis [7] and cancer chemo-prevention and treatment [8].Quercetin acts as strong antioxidant by scavenging free radicals and transition metal ions, thus decreasing the process of lipid peroxidation, which is responsible for the development of many diseases, e.g., cardiovascular and neurodegenerative diseases, as well as liver damage [9][10][11].However, quercetin therapeutic applications present challenges due to (i) low aqueous solubility, (ii) photo and oxidative degradability, (iii) high first-pass effect, (iv) poor intestinal absorption and, hence, low systemic...

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“…When dispersed in an appropriate solvent, gelling agents form a colloidal network structure. 9,10 Lipophilic and hydrophilic drugs can be entrapped in proniosomes either in aqueous layer or in vesicular membrane, which produced chemically and physically stable vesicles having low toxicity because of their non-ionic nature .…”

Section: Introductionmentioning

confidence: 99%

Development of Proniosomal Gel: in-vitro, ex-vivo and in-vivo Characterization

Farooqui¹,

Kar²,

Singh³

et al. 2017

IJPER

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The aim of the present research work was to characterize the ex-vivo, in-vitro and in-vivo studies of proniosomal (PN) gel of ketorolac tromethamine (KT). Experimental work: Proniosomal suspension was prepared by rotatory flask evaporator with addition of nonionic surfactant (Sodium Cholate) at concentration ranges (3%, 2% and 1%). Co-solvent like isopropanol, butanol and ethanol as well as dimethyl sulphoxide (DMSO), was later added which act as permeability enhancers in gel formulations. Carbopol 940 was added as the gelling agent in proniosomal suspension. Characterization: PN gel acts as percutaneous enhancers on the transdermal permeability hence were investigated for ex-vivo (Franz Diffusion Cell), in-vitro (Membrane Diffusion Technique) and in-vivo (Estimation of KT in serum at different time intervals by RP-HPLC) studies. Effect of KT on acute inflammation was evaluated in rat carrageenan-induced edema model. Results: Proniosomal gel formulation F1 consisting of sodium cholate, isopropanol and soya lecithin, showed highest drug release of 94.048 % in 24 hrs and formulation F9 showed lowest drug release of 73.789 % in 16 hrs. Transdermal flux (J) of formulation F1 was found to be high (7.518±0.041µg/cm 2 .hr) as compared to other formulations and marketed preparation. Proniosomal formulation (F1), consisting of sodium cholate (concentration 3%) and cosolvent (isopropanol) attained highest penetrability effect, where sodium cholate and isopropanol induced significant changes in membrane permeability as they completely solubilised membrane phospholipids by sodium cholate micelles. In case of F1 formulation, percent inhibition was found to be 66.84%. Serum estimation of Ketorolac Tromethamine (KT) revealed that application of F1formulation produced 4-fold increase in peak plasma concentration within 12 hours and was maintained upto 24 hours as compared to marketed formulation. Eventually a significant in-vitro-in-vivo correlation was achieved and PN formulation of KT shows significant improvement in bioavailability of KT in systemic circulation when applied via topical route as compared to marketed gel preparation.

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In VitroandIn VivoEvaluation of Niosomal Formulation for Controlled Delivery of Clarithromycin

Cited by 96 publications

References 28 publications

In Vitro in Vivo Evaluation of Niosomal Formulation of Famotidine

In Vitro in Vivo Evaluation of Niosomal Formulation of Famotidine

Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

Development of Proniosomal Gel: in-vitro, ex-vivo and in-vivo Characterization

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