Rutin-encapsulated chitosan nanoparticles targeted to the brain in the treatment of Cerebral Ischemia

Ahmad, Niyaz; Ahmad, Rizwan; Naqvi, Atta Abbas; Alam, Md. Aftab; Ashafaq, Mohammad; Samim, Mohd; Iqbal, Zeenat; Ahmad, Farhan Jalees

doi:10.1016/j.ijbiomac.2016.06.001

Cited by 116 publications

(115 citation statements)

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“…The shape of particles was determined by scanning electron microscopy (SEM) (FEI, INSPECT S50, Czech Republic). The proposed method was adopted from Ahmad et al [28,34].…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

“…Nowadays, chitosan exhibited a mucoadhesive nature, which attracted great attention in different fields like protein and metal adsorption [27,28,33]. Coating on the NPs' surface by chitosan (CS) has been shown to be useful in many applications like a sustained release of drug delivery, with mucoadhesive properties resulting in the enhancement of the drug absorption and prolonged release of drugs [28,34,35], decreasing the burst release of drugs because of the surface modification, and also enhancing the permeation and retention of NPs. This mechanism occurs because of the interest taken between the positively-charged CS and negatively-charged membrane [28,34,35].…”

Section: Introductionmentioning

confidence: 99%

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Quantification and Evaluations of Catechin Hydrate Polymeric Nanoparticles Used in Brain Targeting for the Treatment of Epilepsy

et al. 2020

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To formulate novel chitosan (CS)-coated–PLGA–nanoparticles (NPs) using a central composite design approach and use them in order to improve brain bioavailability for catechin hydrate (CH) through direct nose-to-central nervous system (CNS) delivery for the evaluation of a comparative biodistribution study of CH by the newly developed ultra high performance liquid chromatography mass spectroscopy and mass spectroscopy (UHPLC-MS/MS) method in the treatment of epilepsy. For PLGA–NPs’ preparation, a double emulsion-solvent evaporation method was used, where a four-factor, three-level central composite design was used to obtain the best nanoformulation. For the optimization, four independent variables were chosen, that is, PLGA, polyvinyl alcohol (PVA), sonication time, and temperature. The optimized PLGA–NPs were further coated with chitosan and assessed for drug release, nasal permeation study, as well as a comparative pharmacokinetic and pharmacodynamic study. Independent and dependent variables helped to optimize the best nanoformulation based on the composition of PLGA (50.0 mg), PVA (1.10%), sonication time (90.0 s), and temperature (25.0 °C). The values of dependent variables were observed, such as polydispersity index (PDI), particle size, and zeta potential (ZP)—that is, 0.106 ± 0.01, 93.46 ± 3.94 nm, and −12.63 ± 0.08 mV, respectively. The ZPs of CS-coated PLGA–NPs were changed from negative to positive value with some alteration in the distribution of particle size. Excellent mucoadhesive-nature of CS–CH–PLGA–NPs as compared with CH–S and CH–PLGA–NPs was seen, with a retention time of 0.856 min and m/z of 289.23/245.20 for CH, together with a retention time of 1.04 min and m/z of 301.21/151.21 for Quercetin as an internal standard (IS). For a linear range (1–1000 ng mL−1), % accuracy (93.07–99.41%) and inter- and intraday % precision (0.39–4.90%) were determined. The improved Cmax with area under curve (AUC)0–24 was found to be highly significant (p < 0.001) in Wistar rats’ brain as compared with the i.n. and i.v. treated group based on the pharmacokinetics (PK) results. Furthermore, CS–CH–PLGA–NPs were found to be more significant (p < 0.001) for the treatment of seizure threshold rodent models, that is, increasing current electroshock and pentylenetetrazole-induced seizures. A significant role of CS–CH–PLGA–NPs was observed, that is, p < 0.001, for the enhancement of brain bioavailability and the treatment of epilepsy.

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“…The shape of particles was determined by scanning electron microscopy (SEM) (FEI, INSPECT S50, Czech Republic). The proposed method was adopted from Ahmad et al [28,34].…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Quantification and Evaluations of Catechin Hydrate Polymeric Nanoparticles Used in Brain Targeting for the Treatment of Epilepsy

et al. 2020

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“…Additionally, few studies report the use of natural polymers for nanoencapsulation of rutin (Ahmad et al, 2016;Konecsni, Low, Nickerson, 2012;Oliveira et al, 2016, Zhang, Han, 2018. Bovine serum albumin (BSA) is a non-toxic, biodegradable, and low-cost natural polymer with great potential as a carrier in food and pharmaceutical applications (Jahanshahi, Najafpour, Rahimnejad, 2008;Jun et al, 2011;Wang et al, 2016a).…”

Section: Introductionmentioning

confidence: 99%

Bovine serum albumin-based nanoparticles containing the flavonoid rutin produced by nano spray drying

Pedrozo

Antônio

Khalil

et al. 2020

Braz. J. Pharm. Sci.

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Rutin is a flavonoid compound obtained from different vegetables and fruits; specifically, it is found in the seeds of buckwheat and in fruit peels, particularly citrus. It is also an important constituent of red wine. Rutin exhibits various biological properties including antiviral, vasoprotective, anti-inflammatory, and anticarcinogenic activities. However, its antioxidant activity is the most well studied. Despite the potential for in vitro applications, rutin presents low oral bioavailability that affects its biological activities. Nanoparticles composed of polymers, protein, or lipids are of great importance in the pharmaceutical and nutraceutical areas due to their physicochemical properties, which improve the pharmacokinetics of the drug which is loaded within. This study presents the production of bovine serum albumin (BSA) nanoparticles containing rutin by nano spray drying. Nanoparticles were characterized in terms of mean particle size, size distribution, morphology, zeta potential, and drug content; as well as their antioxidant activity. The optimized spray-drying conditions produced spherical particles with a mean size of 316 nm, zeta potential of −32 mV, and encapsulation efficiency around 32%. Moreover, when antioxidant activity toward the ABTS + radical was assayed, nanoencapsulation increased the IC 50 of rutin by 2-fold. The nano spray-drying process proved to be suitable for the production of rutin-loaded BSA nanoparticles with potential antioxidant activity.

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“…Evidence also shows that mechanism intended to protect rutin from biological degradation and efflux improves the bioavailability of the drug . Despite the positive effects shown by HEE and BF on rutin permeability, BF presented a high ER and HEE the greatest rate of metabolism; therefore, it is unclear whether these preparations could increase the bioavailability of the drug in vivo .…”

Section: Discussionmentioning

confidence: 99%

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces fromPhysalis peruvianaL. on the biopharmaceutics classification of rutin

Moré

Feltrin

Brambila

et al. 2020

Journal of Pharmacy and Pharmacology

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Objectives The Biopharmaceutics Classification System (BCS) categorizes active pharmaceutical ingredients according to their solubility and permeability properties, which are susceptible to matrix or formulation effects. The aim of this research was to evaluate the matrix effects of a hydroethanolic extract of calyces from Physalis peruviana L. (HEE) and its butanol fraction (BF), on the biopharmaceutics classification of their major compound, quercetin‐3‐O‐rutinoside (rutin, RU). Methods Rutin was quantified by HPLC‐UV, and Caco‐2 cell monolayer transport studies were performed to obtain the apparent permeability values (Papp). Aqueous solubility was determined at pH 6.8 and 7.4. Key findings The Papp values followed this order: BF > HEE > RU (1.77 ± 0.02 > 1.53 ± 0.07 > 0.90 ± 0.03 × 10−5 cm/s). The lowest solubility values followed this order: HEE > RU > BF (2.988 ± 0.07 > 0.205 ± 0.002 > 0.189 ± 0.005 mg/ml). Conclusions According to these results, rutin could be classified as BCS classes III (high solubility/low permeability) and IV (low solubility/low permeability), depending on the plant matrix. Further work needs to be done in order to establish how apply the BCS for research and development of new botanical drugs or for bioequivalence purposes.

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Rutin-encapsulated chitosan nanoparticles targeted to the brain in the treatment of Cerebral Ischemia

Cited by 116 publications

References 60 publications

Quantification and Evaluations of Catechin Hydrate Polymeric Nanoparticles Used in Brain Targeting for the Treatment of Epilepsy

Quantification and Evaluations of Catechin Hydrate Polymeric Nanoparticles Used in Brain Targeting for the Treatment of Epilepsy

Bovine serum albumin-based nanoparticles containing the flavonoid rutin produced by nano spray drying

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces fromPhysalis peruvianaL. on the biopharmaceutics classification of rutin

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