Quality by design approach to understand the process of optimization of iloperidone nanostructured lipid carriers for oral bioavailability enhancement

Mandpe, Leenata; Pokharkar, Varsha

doi:10.3109/10837450.2013.867445

Cited by 51 publications

(13 citation statements)

References 15 publications

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“…It was observed that increased lipid concentration, the EE increases because of more space available for housing as well as minimized escaping of drug to external phase. This result agreed to previously published work i.e., optimization of oral NLCs delivery of isradipine 35 , iloperidone 36 and carvedilol 37 . On increasing surfactant concentration the EE increased, because it increases viscosity of aqueous phase, thus dispersion of drug into external phase decreases.…”

Section: Oral Lipid Based Nano-formulation Of Dapagliflozinsupporting

confidence: 93%

“…4. The DG-NLCs-opt exhibited dual release pattern, initial fast release 21.3 3.12 in 1 h followed by slow and prolonged release 90.01 2.01 whereas DG-dispersion showed 31.54 1.87 release in 24 h. Initial fast release is due to presence of DG on NLCs surface and slow is due to erosion or degradation of lipid core matrix 36 Hixon-Crowell model 0.9383 zero-order 0.8283 . Maximum R 2 was found for Korsmeyer-Peppas model and selected as best fitted kinetic model.…”

Section: In Vitro Release Studymentioning

confidence: 95%

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Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, in vitro Characterization and ex vivo Intestinal Permeation Study

Zafar

2020

J. Oleo Sci.

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IntroductionDiabetes type 2, diabetes mellitus is a group of metabolic disease in which the blood glucose level increase ≥ 200 mg/dL for a long period. Due to high blood glucose level, many other symptoms appeared simultaneously like more frequent urination, weight loss, increased hunger, dehydration, as well as the alteration in lipid profile, liver function test and kidney function test. The associated complication may occur like heart attack, kidney failure and damaged eye in chronic and serious condition. In worldwide approx. 422 million peoples were affected and about 1.6 million deaths occurred in the low and middle-income countries in every year 1 . Various oral dosage form available in the market to reduce the blood glucose level

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Section: Oral Lipid Based Nano-formulation Of Dapagliflozinsupporting

confidence: 93%

Section: In Vitro Release Studymentioning

confidence: 95%

Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, in vitro Characterization and ex vivo Intestinal Permeation Study

Zafar

2020

J. Oleo Sci.

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“…The optimized NGN-NLC formulation was subjected to dilution following the addition of a drop of the NGN-NLC on a copper grid coated with carbon, which was then dried and negatively stained with 1% phosphotungstic acid. The grid was then placed in the instrument and examined by TEM [ 46 ].…”

Section: Methodsmentioning

confidence: 99%

Thymoquinone-Enriched Naringenin-Loaded Nanostructured Lipid Carrier for Brain Delivery via Nasal Route: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Treatment of Depression

et al. 2022

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In the current research, a thymoquinone-enriched naringenin (NGN)-loaded nanostructured lipid carrier (NLC) was developed and delivered via the nasal route for depression. Thymoquinone (TQ) oil was used as the liquid lipid and provided synergistic effects. A TQ- and NGN-enriched NLC was developed via the ultrasonication technique and optimized using a central composite rotatable design (CCRD). The optimized NLC exhibited the following properties: droplet size, 84.17 to 86.71 nm; PDI, 0.258 to 0.271; zeta potential, −8.15 to −8.21 mV; and % EE, 87.58 to 88.21%. The in vitro drug release profile showed the supremacy of the TQ-NGN-NLC in comparison to the NGN suspension, with a cumulative drug release of 82.42 ± 1.88% from the NLC and 38.20 ± 0.82% from the drug suspension. Ex vivo permeation study displayed a 2.21-fold increase in nasal permeation of NGN from the NLC compared to the NGN suspension. DPPH study showed the better antioxidant potential of the TQ-NGN-NLC in comparison to NGN alone due to the synergistic effect of NGN and TQ oil. CLSM images revealed deeper permeation of the NGN-NLC (39.9 µm) through the nasal mucosa in comparison to the NGN suspension (20 µm). Pharmacodynamic studies, such as the forced swim test and the locomotor activity test, were assessed in the depressed rat model, which revealed the remarkable antidepressant effect of the TQ-NGN-NLC in comparison to the NGN suspension and the marketed formulation. The results signify the potential of the TQ-enriched NGN-NLC in enhancing brain delivery and the therapeutic effect of NGN for depression treatment.

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“…Also, it shows high first-pass metabolism [5]. Solubility of Ilo has been enhanced by microspheres, binary, ternary complexation with cyclodextrins, self-emulsifying preconcentrate, whereas bioavailability of Ilo has been improved by co-crystallization, sublingual film, and nanolipid carriers [5][6][7][8][9][10]. Among them, oral administration is mostly preferred as it advantageous compared with other routes of administration.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Sublingual Tablets of Iloperidone Prepared by Microenvironmental pH Regulated Approach

2020

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Purpose Iloperidone (Ilo) is an antipsychotic drug having low and pH-dependent solubility, hence less bioavailability. Thus, the aim of this study was to prepare and characterize binary (TAPOL B) and ternary complexes (TAPOL T) of drug with Kolliphor P-188 and tartaric acid to improve solubility. Further, sublingual tablets incorporating ternary complex were formulated to improve the dissolution. Methods Preliminary screening studies were conducted to select the acidifying agent and polymer based on saturation solubility studies. Binary and ternary complexes were prepared by the melting method. Complexes were characterized by DSC, powder Xray diffraction (PXRD), FTIR, microenvironmental studies, and in vitro dissolution studies. The sublingual tablets of ternary complexes were prepared by the direct compression method and evaluated for weight variation, disintegration time, and dissolution studies. Results Based on solubility studies, Kolliphor P-188 and tartaric acid were selected as polymer and acidifying agents. DSC studies and FTIR spectra showed the interaction of drugs with polymer and acidifying agents. PXRD spectra showed the crystalline nature of complexes. Microenvironmental studies carried out in pH 6.8 showed a drastic decrease in pH with ternary complex as compared with binary complex. Dissolution studies showed an increase in dissolution, TAPOL T > TAPOL B > drug. The sublingual tablets showed disintegration time < 30 s and more than 80% of a drug released within 10 min. Due to the presence of tartaric acid and polymer, solubility of the drug increases tremendously.Conclusion The present study demonstrates the increase in solubility and release of Iloperidone due to the microenvironmental pH effect from sublingual tablets. Hence, microenvironmental pH modification is a good approach to increase drug solubility and dissolution. Keywords Iloperidone . Tartaric acid . Kolliphor P-188 . Ternary complex . Microenvironmental pH . Sublingual tablets Highlights • Binary and ternary complexes of Ilo were formulated.• Kolliphor P-188 and tartaric acid were optimized as a polymer and an auxiliary agent. • Tartaric acid accelerated the dissolution efficiency of the drug due to pH change. • DC tablets showed ≥ 80% release within 5 min for 12 mg, maximum strength.

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Quality by design approach to understand the process of optimization of iloperidone nanostructured lipid carriers for oral bioavailability enhancement

Abstract: The NLC formulation remarkably improved the oral bioavailability of ILO and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs.

Cited by 51 publications

References 15 publications

Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, <i>in vitro</i> Characterization and <i>ex vivo</i> Intestinal Permeation Study

Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, <i>in vitro</i> Characterization and <i>ex vivo</i> Intestinal Permeation Study

Thymoquinone-Enriched Naringenin-Loaded Nanostructured Lipid Carrier for Brain Delivery via Nasal Route: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Treatment of Depression

Formulation and Characterization of Sublingual Tablets of Iloperidone Prepared by Microenvironmental pH Regulated Approach

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