Process optimization by response surface methodology for preparation and evaluation of methotrexate loaded chitosan nanoparticles

Naveen, N. Raghavendra; Kurakula, Mallesh; Gowthami, Buduru

doi:10.1016/j.matpr.2020.01.491

Cited by 51 publications

(18 citation statements)

References 26 publications

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“…All the responses observed were concurrently fitted to different models. The best fitting experimental model (main, interaction and quadratic) was taken statistically based on a comparison of several statistical parameters like coefficient of variation (CV), multiple correlation coefficient (R 2 ), adjusted R 2 (Adju.R 2 ) and predicted R 2 (Pred.R 2 ) [36]. The level of significance was considered at p-values < 0.05.…”

Section: Optimization Of Sim-qrc Npsmentioning

confidence: 99%

In Situ Gel Loaded with Chitosan-Coated Simvastatin Nanoparticles: Promising Delivery for Effective Anti-Proliferative Activity against Tongue Carcinoma

Kurakula

Naveen²

2020

Marine Drugs

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The goal of this study is to develop optimized chitosan-coated Simvastatin (SIM) nanoparticles (NPs) loaded in an in situ gel (ISG) formulation via a face-centered central composite design (FCCCD). Coated SIM-NPs were doped with Quercetin (QRC) using a modified nanoprecipitation method. The concentrations of poloxamer 188 (A) and chitosan (B) at five different levels, plus/minus alpha (+1.414 and −1.414: axial points), plus/minus 1 (factorial points) and the center point were optimized for particle size (PS-Y1), entrapment efficacy (EE-Y2) and stability index (SI-Y3). Based on the desirability approach, a formulation containing poloxamer 188 0.24% and chitosan 0.43% renders the prerequisites of optimum formulation for preparing SIM-QRC NP-loaded ISG. Scanning microscopy showed spherical SIM-NPs, indicating monodispersity in the range of 0.50 ± 0.04 nm with a charge of +32.42 mV. The optimized formulation indicated the highest EE 79.67% and better stability at 4 • C. Drug release from SIM-QRC NP-loaded ISG was slower to plateau by up to 96 h and, at the end of 168 h, only 65.12% of SIM was released in a more controlled manner in comparison to SIM-QRC NPs and plain SIM. ISG formulation showed a considerable increase in apoptosis occurrence through caspase-3 mediation and it also enhanced the tumor suppressor protein levels. Enhanced biological activity of SIM was observed due to QRC enabling promising drug and polymer synergistic interaction. The proposed formulation can provide a breakthrough in localized therapy, overcoming the potential drawbacks of systemic chemotherapy for tongue carcinoma.

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Section: Optimization Of Sim-qrc Npsmentioning

confidence: 99%

In Situ Gel Loaded with Chitosan-Coated Simvastatin Nanoparticles: Promising Delivery for Effective Anti-Proliferative Activity against Tongue Carcinoma

Kurakula

Naveen²

2020

Marine Drugs

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“…Therefore, it is crucial to rigorously characterize CS in order to design the most optimal formulation for a specific purpose. To further optimize the suitability of CS-based nanocarriers as delivery systems, it is essential to characterize them for their physicochemical properties and understand them on a molecular level [15,47]. Thus, we characterized the nanocapsules regarding their physicochemical properties.…”

Section: Highly Monodisperse and Positively Charged Nanocapsules Succmentioning

confidence: 99%

Capsaicin-Loaded Chitosan Nanocapsules for wtCFTR-mRNA Delivery to a Cystic Fibrosis Cell Line

et al. 2020

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Cystic fibrosis (CF), a lethal hereditary disease caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene coding for an epithelial chloride channel, is characterized by an imbalanced homeostasis of ion and water transports in secretory epithelia. As the disease is single-gene based, transcript therapy using therapeutic mRNA is a promising concept of treatment in order to correct many aspects of the fatal pathology on a cellular level. Hence, we developed chitosan nanocapsules surface-loaded with wtCFTR-mRNA to restore CFTR function. Furthermore, we loaded the nanocapsules with capsaicin, aiming to enhance the overall efficiency of transcript therapy by reducing sodium hyperabsorption by the epithelial sodium channel (ENaC). Dynamic light scattering with non-invasive back scattering (DLS-NIBS) revealed nanocapsules with an average hydrodynamic diameter of ~200 nm and a Zeta potential of ~+60 mV. The results of DLS-NIBS measurements were confirmed by asymmetric flow field-flow fractionation (AF4) with multidetection, while transmission electron microscopy (TEM) images confirmed the spherical morphology and size range. After stability measurements showed that the nanocapsules were highly stable in cell culture transfection medium, and cytotoxicity was ruled out, transfection experiments were performed with the CF cell line CFBE41o-. Finally, transepithelial measurements with a new state-of-the-art Ussing chamber confirmed successfully restored CFTR function in transfected cells. This study demonstrates that CS nanocapsules as a natural and non-toxic delivery system for mRNA to target cells could effectively replace risky vectors for gene delivery. The nanocapsules are not only suitable as a transcript therapy for treatment of CF, but open aspiring possibilities for safe gene delivery in general.

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“…Apart from all these novel systems, nanowires, nanofibers, nanoethanosomes and nanofilms are gained their importance in enhancing the oral bioavailability of poorly soluble drugs [33][34][35][36][37][38] . Though the optimizing of several parameters in preparing optimum nano-formulation is bit complicated, several applications like quality by design/ response surface methodology or PAT can be successfully applied [39][40][41][42][43][44] .…”

Section: Novel Technologies In Delivery Of Poorly Soluble Drugsmentioning

confidence: 99%

Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs

Gowthami

Krishna²,

Rao

2020

Int. J. Res. Pharm. Sci & Tech.

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Oral administration is considered as major, convenient route among all other routes of delivery, owing to several benefits. But, the poor solubility or enzymatic/metabolic activity are the major concerns in developing a successful formulation. About 40% of approved drugs which are in the current market and 90% of new drug molecules in the developmental pipeline are hydrophobic in nature. The challenge to formulate insoluble drugs has met with various approaches to overcome the problems related to solubility, application of nanotechnology is one amongst them. The present review deals with various nanocarriers and technologies that are proven to be effective in enhancing the bioavilability of poorly soluble drugs.

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Process optimization by response surface methodology for preparation and evaluation of methotrexate loaded chitosan nanoparticles

Cited by 51 publications

References 26 publications

In Situ Gel Loaded with Chitosan-Coated Simvastatin Nanoparticles: Promising Delivery for Effective Anti-Proliferative Activity against Tongue Carcinoma

In Situ Gel Loaded with Chitosan-Coated Simvastatin Nanoparticles: Promising Delivery for Effective Anti-Proliferative Activity against Tongue Carcinoma

Capsaicin-Loaded Chitosan Nanocapsules for wtCFTR-mRNA Delivery to a Cystic Fibrosis Cell Line

Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs

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