Formulation and biopharmaceutical evaluation of risperidone-loaded chitosan nanoparticles for intranasal delivery

Rajalakshmi, R.; Muzib, Y. Indira; Yalavarthi, Prasanna Raju

doi:10.1080/03639045.2019.1619759

Cited by 42 publications

(26 citation statements)

References 36 publications

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“…Response surface graphs were generated using polynomial equations, which represented simultaneous effect of two variables on response parameters by taking one variable at a constant level. Increased EE with increased chitosan (X 1 ) could be attributed to more amount of chitosan that had higher ability to form ionic gel with increased viscosity of dispersion thereby increased diffusional resistance of guggul to move forward into external phase through polymer droplet [16]. Moreover, time required for polymer precipitation decreased at higher polymer concentration and rapidly precipitated on the surface of dispersed phase, which prevented guggul molecules to diffuse out of GNPs across the phase boundary.…”

Section: Discussionmentioning

confidence: 99%

“…Measurements were performed by dynamic light scattering technique with scattering angle of 90° at 25 ± 0.5°C. [16] Morphology of optimized GNPs was analysed by high resolution scanning electron microscope (Carl Zeiss Merlin Compact, Chennai). For that, the GNPs sample was placed on an aluminium stub, dried under vacuum and then sputtered with gold.…”

Section: Particle Size Zeta Potential and Morphologymentioning

confidence: 99%

“…Among different approaches explored so far, colloidal carriers are of particular interest, especially those made from natural polymers [15]. Among biopolymers, chitosan is one of the most promising coating materials for many bioactive agents due to its nontoxic, biocompatible, and biodegradable characteristics [16,17]. In this context, the present research was aimed to design and optimize guggul loaded chitosan nanoparticles (GNPs) by ionic gelation method, optimized by a Box-Behnken Design (BBD), and to improve the release characteristics and antihyperlipidemic potential.…”

Section: Introductionmentioning

confidence: 99%

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Design of Guggul Lipid Loaded Chitosan Nanoparticles Using Box-Behnken Design – An Evaluation Study

Murthy

Yelavarthi

Devanna

et al. 2021

JPRI

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Aim: Guggul lipid, a lipophillic antihyperlipidemic moiety, undergoes extensive first-pass metabolism and has low bioavailability. In order to address this limitation, guggul lipid loaded chitosan nanoparticles (GNPs) were designed, optimized and processed by 3- factor 3- level Box- Behnken design (BBD). Methodology: A 3-factor 3-level BBD was employed to investigate combined influence of formulation variables on percent entrapment efficiency (EE) and percent drug release (DR) of GNPs prepared by ionic gelation method. The generated polynomial equation was validated and desirability function was utilized for optimization. Optimized GNPs were evaluated for physicochemical, morphological, release characteristics, solid state characterization and in-vitro cell line studies. Results: Amounts of chitosan, sodium tripolyphosphate and guggul were selected as independent variables had variably influenced EE and DR. Optimized GNPs were produced with an average size of 96.5 nm, electro kinetic potential of -15.4 mV, EE of 92.98% and DR of 95.12% in 24 h with sustained release. Physicochemical and in-vitro characterization revealed existence of guggul in amorphous form in GNPs without interaction and exhibited sustained release profile following first order with Higuchi kinetics. GNPs possessed lipase inhibition activity with IC50 value of 14.72 µg/ml and better viability against various cell lines with CTC50 values (256.24 to 321.27 µg/ml). Conclusions: Design and optimization of GNPs by BBD proved to be an effective and promising approach. High entrapment of guggul followed controlled release were the outcomes of GNPs prepared by ionic gelation with improved cell viability.

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Section: Discussionmentioning

confidence: 99%

Section: Particle Size Zeta Potential and Morphologymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Design of Guggul Lipid Loaded Chitosan Nanoparticles Using Box-Behnken Design – An Evaluation Study

Murthy

Yelavarthi

Devanna

et al. 2021

JPRI

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“…Before lyophilization, the suspension was centrifuged at 10,000 rpm for 15 min using centrifuge (REMI Centrifuge, Mumbai, India). The supernatant was separated, filtered, and quantified by UV spectrophotometer at 205 nm [21]. The EE was calculated from following equation.…”

Section: Entrapment Efficiency (%Ee)mentioning

confidence: 99%

Process of Orlistat-Loaded Chitosan Nanoparticles Using Box–behnken Design – An Evaluation Study

Yelavarthi

Devanna

2021

Asian J Pharm Clin Res

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Objective: High lipophilicity and extensive hepatic metabolism limit oral application of orlistat in obesity treatment. Orlistat-loaded chitosan nanoparticles (CONPs) were optimized by 3-factor 3-level Box–Behnken design (BBD) and surfaced engineered to address limitations. Methods: CONPs were prepared by ionic gelation method. Amounts of chitosan (X1), sodium tripoly phosphate (X2), and orlistat (X3) were selected as independent factors, whereas % entrapment efficiency (Y1) and % drug release (Y2) were employed as responses in BBD. Three-dimensional response surface plots were run to understand the main interaction and quadratic effects of independent variables. Further optimized formulation was surface engineered by Eudragit L-100 (ECONPs) and characterized by FTIR, DSC, XRD, particle size, zeta potential, and SEM. Entrapment efficiency, release kinetics, stability, and in vitro cell line studies were carried out. Results: ECONPs were produced with an average size of 534.6 nm, zeta potential of +5.7 mV, EE of 78.62%, and DR of 80.86%. Eudragit coated CONPs anchored the release of orlistat at pH 6.8 desirable for duodenal targeting. Orlistat was released with low, burst, and sustained release manner over 24 h period followed first-order kinetics with Higuchi model with drug content of 84.87% and 78.44% of release. ECONPs possessed lipase inhibition with IC50 value of 8.0 μg/ml and viability against selected cell lines with CTC50 values (26.32–32.21 μg/ml). Conclusion: BBD was a promising tool in elucidating the insights of formulation variables of CONPs. ECONPs fulfilled the rationale of orlistat release, lipase inhibition, and viability against selected cell lines.

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“…Recent studies showed several potential psychiatric drug delivery systems using poly (lactic- co -glycolic acid) (PLGA) [ 26 ], a polyelectrolyte complexation between dextran-sulfate and dextran-chitosan [ 27 ] and solid lipids such as glyceryl monostearate [ 28 ]. Unlike these systems, which may possess disadvantages such as polymer growth, polydisperse distributions, bio-changes, toxicity, side effects, and high cost, the proteinoid nanocarriers presented in this study are biodegradable, non-toxic, and non-immunogenic.…”

Section: Introductionmentioning

confidence: 99%

Proteinoid Nanocapsules as Drug Delivery System for Improving Antipsychotic Activity of Risperidone

et al. 2020

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Risperidone (RSP) is an atypical antipsychotic drug widely used to treat schizophrenia and bipolar disorder. Nanoparticles (NPs) are being developed as in vivo targeted drug delivery systems, which cross the blood-brain barrier and improve pharmacokinetics and drug effectiveness. Here, biodegradable proteinoids were synthesized by thermal step-growth polymerization from the amino acids l-glutamic acid, l-phenylalanine and l-histidine and poly (l-lactic acid). Proteinoid NPs containing RSP were then formed by self-assembly, overcoming the insolubility of the drug in water, followed by PEGylation (poly ethylene glycol (PEG) conjugation to increase the stability of the NPs in the aqueous continuous phase. These NPs are biodegradable owing to their peptide and ester moieties. They were characterized in terms of diameter, size distribution, drug loading, and long-term storage. Behavioral studies on mice found enhanced antipsychotic activity compared to free RSP.

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Formulation and biopharmaceutical evaluation of risperidone-loaded chitosan nanoparticles for intranasal delivery

Cited by 42 publications

References 36 publications

Design of Guggul Lipid Loaded Chitosan Nanoparticles Using Box-Behnken Design – An Evaluation Study

Design of Guggul Lipid Loaded Chitosan Nanoparticles Using Box-Behnken Design – An Evaluation Study

Process of Orlistat-Loaded Chitosan Nanoparticles Using Box–behnken Design – An Evaluation Study

Proteinoid Nanocapsules as Drug Delivery System for Improving Antipsychotic Activity of Risperidone

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