A Quality by Design Concept on Lipid Based Nanoformulation Containing Antipsychotic Drug: Screening Design and Optimization using Response Surface Methodology

Patel, Manthan; Sawant, Krutika

doi:10.4172/2157-7439.1000442

Cited by 17 publications

(20 citation statements)

References 16 publications

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“…A central composite design, a type of response surface methodology, was used to statistically optimize critical factors and to estimate main interaction and quadratic effects of factors on critical quality attribute of Lercanidipine loaded nanosuspension [16]. Based on the results obtained from preliminary studies, two critical parameters, polymer concentration (X 1 ) and SAS ratio (X 2 ), were taken as independent variables and their levels were suitably coded as per Table 1.…”

Section: Optimization Using Central Composite Designmentioning

confidence: 99%

An impact of nanocrystals on dissolution rate of Lercanidipine: Supersaturation and crystallization by addition of solvent to antisolvent

Gadhiya

Patel²,

Bagada

2021

Futur J Pharm Sci

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Background Nanocrystals of any drug are pure solid drug particles with a mean diameter in nanometer range. Dissolution is a crucial factor for absorption of medicine in case of water-insoluble or poorly soluble drugs. The aim of this study was to develop nanocrystals of a hydrophobic drug, Lercanidipine, by addition of solvent to an antisolvent with high-speed homogenization to achieve dissolution and solubility enhancement. Addition of organic solvent to antisolvent results in genesis of nanosized particles due to fast nucleation process and rapid mixing. The nanosuspension was formulated using PVP K30 as a stabilizer. Further, nanosuspensions were lyophilized to convert into solid nanocrystals using mannitol as a cryoprotectant. The developed nanosuspensions were characterized for particle size, zeta potential, saturation solubility, and in vitro dissolution studies. Lyophilized solid nanocrystals were characterized for FTIR, SEM, XRD, and zeta potential (ζ). Results Central composite design was executed to study influence of amount of stabilizer and solvent to antisolvent ratio (independent variables) on particle size and % drug release at 10 min (dependent variables). The particle size of the developed Lercanidipine nanosuspensions were observed in the range of 302.00 ± 10.58 to 484.33 ± 6.51 nm measured by Zetatrac. A considerable increase was found in the solubility and dissolution rate of the nanocrystals as compared to pure drug. The drug release from Lercanidipine nanosuspensions was increased up to 88.95% within 10 min as compared to pure Lercanidipine which was only 21.53%. The X-ray diffraction study of lyophilized nanocrystals showed sharp and distinct peaks due to an increse in crystallinity of Lercanidipine Particle morphology was studied by scanning electron microscopy revealed that nanoprecipitated particles with lyophilization in the presence of mannitol exhibited dendrite needle-like crystals. Conclusion The nanocrystal development by antisolvent precipitation procedure using methanol as solvent, water as antisolvent, and low amounts of PVP K30 as stabilizer is a very promising and effective method to increase the dissolution rate of Lercanidipine. Graphical abstract

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Section: Optimization Using Central Composite Designmentioning

confidence: 99%

An impact of nanocrystals on dissolution rate of Lercanidipine: Supersaturation and crystallization by addition of solvent to antisolvent

Gadhiya

Patel²,

Bagada

2021

Futur J Pharm Sci

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“…Design space is referred as the multidimensional combination and interaction of input variables and process parameters that have been demonstrated to provide assurance of quality [45] and was obtained by overlaying the critical response contours with overlay plot (Figure 4). The yellow coloured regions describe the design space with suitable response values and grey regions illustrate where response values did not meet the quality product attributes.…”

Section: Design Spacementioning

confidence: 99%

Impact of liquid lipid on development and stability of trimyristin nanostructured lipid carriers for oral delivery of resveratrol

Houacine

Adams

Singh

2020

Journal of Molecular Liquids

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“…This lipid phase was dispersed in the aqueous surfactant solution (2.5% of Poloxamer 188 and 0.02% of D-a-TPGS) at 70 C using a homogenizer (T-25 digital Ultra-Turrax, IKA India Private Limited, Bengaluru, India). The resultant emulsion was ultrasonicated using a probe sonicator (Labsonic, Sartorius, Germany) and cooled in an ice bath [6,7]. The obtained AM-SLNs were lyophilized using trehalose in the ratio of 1:3 with respect to solid content [8].…”

Section: Preparation Of Am Loaded Slnsmentioning

confidence: 99%

“…Detailed characterization of the AM-SLNs has been described previously [6]. The particle size (PS) and zeta potential of the SLNs were measured using Zetasizer (Malvern, UK).…”

Section: Physicochemical Characterization Of Am-slnsmentioning

confidence: 99%

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Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies

Patel

Mundada

Sawant

2019

Artificial Cells, Nanomedicine, and Biotechnology

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The aim of the present investigation was to fabricate and evaluate solid lipid nanoparticles (SLNs) of asenapine maleate (AM) to improve its oral bioavailability (BA). AM-SLNs were prepared by high speed homogenization followed by ultrasonication technique. The resultant SLNs exhibited particle size, zeta potential and entrapment efficiency of 114.3 ± 3.5 nm, À12.9 ± 3.8 mV, and 84.10% ± 2.90% respectively. In vitro release study of AM-SLNs showed 9.23% ± 2.72% and 92.09% ± 3.40% release of AM in pH 1.2 medium and phosphate buffer pH 6.8, respectively, indicating higher potential of lymphatic uptake. Cell viability study using Caco-2 cell line indicated non-toxicity of the carriers and drug. The uptake of AM-SLNs across Caco-2 cell line was time and energy dependent exhibiting clathrin-claveole mediated endocytosis transport. Cellular uptake of Coumarin loaded SLNs was effectively increased as compared to the dye solution. The pharmacokinetic results in rats showed 50.19-fold improvement in BA of AM after fabrication of SLNs. Collectively, all these findings demonstrated effectiveness of SLNs to improve therapeutic efficacy of AM in the treatment of schizophrenia.

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A Quality by Design Concept on Lipid Based Nanoformulation Containing Antipsychotic Drug: Screening Design and Optimization using Response Surface Methodology

Cited by 17 publications

References 16 publications

An impact of nanocrystals on dissolution rate of Lercanidipine: Supersaturation and crystallization by addition of solvent to antisolvent

An impact of nanocrystals on dissolution rate of Lercanidipine: Supersaturation and crystallization by addition of solvent to antisolvent

Impact of liquid lipid on development and stability of trimyristin nanostructured lipid carriers for oral delivery of resveratrol

Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies

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