QbD-based Formulation Optimization and Characterization of Polymeric Nanoparticles of Cinacalcet Hydrochloride with Improved Biopharmaceutical Attributes

Ghose, Debashish; Patra, Chinam Niranjan; Kumar, Bera Varaha Venkata Ravi; Swain, Sanjit Kumar; Jena, Bikash Ranjan; Choudhury, Punam; Shree, Dipthi

doi:10.4274/tjps.galenos.2020.08522

Cited by 14 publications

(6 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Mean particle size, polydispersity index (PDI), and zeta potential of blank and DCX-loaded NPs are presented in Table 1 . The mean particle size of the PLGA NPs was found to be in the range of 247.5–309.6 nm and the PDI ranged from 0.241 to 0.362, which is in the acceptable range (PDI < 0.4) for nanoparticular drug delivery systems [ 41 ]. The zeta potentials of blank and drug-loaded PLGA NPs were found to be −22.4 and −26.1 mV, respectively, while those of CS-coated PLGA NPs were +29.6 and +24.4 mV, respectively.…”

Section: Resultsmentioning

confidence: 99%

Orally administered docetaxel-loaded chitosan-decorated cationic PLGA nanoparticles for intestinal tumors: formulation, comprehensive in vitro characterization, and release kinetics

Ünal¹,

Doğan²,

Aktaş³

2022

Beilstein J. Nanotechnol.

View full text Add to dashboard Cite

Intestinal cancers are the third most lethal cancers globally, beginning as polyps in the intestine and spreading with a severe metastatic tendency. Chemotherapeutic drugs used in the treatment of intestinal tumors are usually formulated for parenteral administration due to poor solubility and bioavailability problems. Pharmaceutically, clinical failure due to a drug’s wide biodistribution and non-selective toxicity is one of the major challenges of chemotherapy. In addition, parenteral drug administration in chronic diseases that require long-term drug use, such as intestinal tumors, is challenging in terms of patient compliance and poses a burden in terms of health economy. Especially in the field of chemotherapy research, oral chemotherapy is a subject that has been intensively researched in recent years, and developments in this field will provide serious breakthroughs both scientifically and socially. Development of orally applicable nanodrug formulations that can act against diseases seen in the distant region of the gastrointestinal tract (GIT), such as intestinal tumor, brings with it a series of difficulties depending on the drug and/or GIT physiology. The aim of this study is to develop an oral nanoparticle drug delivery system loaded with docetaxel (DCX) as an anticancer drug, using poly(lactic-co-glycolic acid) (PLGA) as nanoparticle material, and modified with chitosan (CS) to gain mucoadhesive properties. In this context, an innovative nanoparticle formulation that can protect orally administered DCX from GIT conditions and deliver the drug to the intestinal tumoral region by accumulating in mucus has been designed. For this purpose, DCX-PLGA nanoparticles (NPs) and CS/DCX-PLGA NPs were prepared, and their in vitro characteristics were elucidated. Nanoparticles around 250–300 nm were obtained. DCX-PLGA NPs had positive surface charge with CS coating. The formulations have the potential to deliver the encapsulated drug to the bowel according to the in vitro release studies in three different simulated GIT fluids for approximately 72 h. Mucin interaction and penetration into the artificial mucus layer were also investigated in detail, and the mucoadhesive and mucus-penetration characteristics of the formulations were examined. Furthermore, in vitro release kinetic studies of the NPs were elucidated. DCX-PLGA NPs were found to be compatible with the Weibull model, and CS/DCX-PLGA NPs were found to be compatible with the Peppas–Sahlin model. Within the scope of in vitro cytotoxicity studies, the drug-loaded NPs showed significantly higher cytotoxicity than a DCX solution on the HT-29 colon cell line, and CS/DCX-PLGA showed the highest cytotoxicity (p < 0.05). According to the permeability studies on the Caco-2 cell line, the CS/DCX-PLGA formulation increased permeability by 383% compared to free DCX (p < 0.05). In the light of all results, CS/DCX-PLGA NPs can offer a promising and innovative approach as an oral anticancer drug-loaded nanoformulation for intestinal tumors.

show abstract

Section: Resultsmentioning

confidence: 99%

Orally administered docetaxel-loaded chitosan-decorated cationic PLGA nanoparticles for intestinal tumors: formulation, comprehensive in vitro characterization, and release kinetics

Ünal¹,

Doğan²,

Aktaş³

2022

Beilstein J. Nanotechnol.

View full text Add to dashboard Cite

show abstract

“…The quality attributes critical to formulating pastilles were chosen as responses to measure in the optimization design. Disintegration time and TDL release were considered critical quality attributes (CQAs) to formulate immediate-release pastilles [ [57] , [58] , [59] ]. QTPPs and CQAs were identified and shown in Table 1 .…”

Section: Methodsmentioning

confidence: 99%

Investigating in-vitro functionality and in-vivo taste assessment of eco-friendly Tadalafil Pastilles

Rana,

Panchal,

Thakkar

et al. 2024

Heliyon

View full text Add to dashboard Cite

“…To compute the independent variables (CMPs) and their capable effects upon the desired critical quality attributes (CQAs), regarded as independent factors such as peak area, retention time (Rt), and USP plate count. The focal, interactions, and quadratic effects of the influential critical method parameters i.e mobile phase ratio, flow rate, and injection volume upon the dependent factors (responses) peak area (Y1), retention time (Y2), USP plate count (Y3), are analyzed with total 17 experimental runs [24][25][26][27]. A method operable design region (MODR) or appropriate design space was earmarked, providing the best method [20], [26], [27].…”

Section: Methods Development Using Box-benkhen Design (Bbd)mentioning

confidence: 99%

Response Surface Methodology Driven Systematic Development of a Stability- indicating RP-UPLC Method for the Quantification of Aliskiren: A Renin Inhibitor

Jena

Rao

Alavala

et al. 2021

JPRI

Self Cite

View full text Add to dashboard Cite

Aims: The current study envisages experimental design enabled rapid, sensitive, and stability-indicating RP-UPLC method to quantify Aliskiren in its pharmaceutical formulations. Study Design: Box-Benkhen experimental Design using Response surface methodology. Place and Duration of Study: Department of Analytical Research and Development, Brawn laboratories ltd., Gurugram, India, and Department of Pharmacy KL College Pharmacy, KL Deemed to be University, Vaddesearam, Guntur, Andhra Pradesh, between May 2021 and September 2021. Methodology: The chromatographic partitioning was achieved on a Waters Acuity H class UPLC system, with BEH 130οA, C18 column (100 x 2.1 mm,1.7 μm) having isocratic elution containing (50:50 %v/v) of 0.2% Glacial acetic acid (GAA) : acetonitrile, at constant flow rate using PDA detection. The optimum conditions were delineated, selecting three influential factors (CMPs), i.e., mobile phase composition, flow rate, and injection volume. Systematic optimization was accomplished by 32 Box-Benkhen design using response surface methodology (RSM). Results: The selected variables are evaluated for obtained responses (CAAs), i.e., peak area, retention time (Rt), USP Plate count. The final optimized method employed, organic phase composition 0.2 % GAA (pH 3.0) and acetonitrile 50:50 (% v/v) with 0.3 mL min-1 flow rate. The injection volume was maintained as 2μL with 2 minutes run time and λmax 280 nm. Conclusion: The method was linear for 5-300 ppm, with regression co-efficient (R2) 0.9995. As per ICH guidelines, forced degradation studies were carried out to analyse the stability profile of drug. The short Rt 1.214, minute implies superior robustness, sensitivity, and cost-effectiveness for routine analysis. The results exhibited that RSM approach of QbD will be competently used to optimize the RP-UPLC method with fewer experimental trials and error-free investigation.

show abstract

QbD-based Formulation Optimization and Characterization of Polymeric Nanoparticles of Cinacalcet Hydrochloride with Improved Biopharmaceutical Attributes

Cited by 14 publications

References 0 publications

Orally administered docetaxel-loaded chitosan-decorated cationic PLGA nanoparticles for intestinal tumors: formulation, comprehensive in vitro characterization, and release kinetics

Orally administered docetaxel-loaded chitosan-decorated cationic PLGA nanoparticles for intestinal tumors: formulation, comprehensive in vitro characterization, and release kinetics

Investigating in-vitro functionality and in-vivo taste assessment of eco-friendly Tadalafil Pastilles

Response Surface Methodology Driven Systematic Development of a Stability- indicating RP-UPLC Method for the Quantification of Aliskiren: A Renin Inhibitor

Contact Info

Product

Resources

About