Formulation and optimization of cilnidipine loaded nanosuspension for the enhancement of solubility, dissolution and bioavailability

Shaikh, Farhatjahan; Patel, Meenakshi; Patel, Vandana B.; Patel, Ashwini; Shinde, Gajanan; Shelke, Santosh; Pathan, Inayat Bashir

doi:10.1016/j.jddst.2021.103066

Cited by 15 publications

(6 citation statements)

References 45 publications

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“…The entrapment efficiency (%EE) of (N4) was better than N8; 95.84667% ± 0.159478 (N4) vs 65.74%± 1.292904 (N8), due to the higher availability of surfactant of SL led to smaller micelles which can accommodate or encapsulate the drug (26) .…”

Section: Entrapment Efficiency Measurement Of Cld Nanoparticlesmentioning

confidence: 96%

Factors affecting the preparation of Cilnidipine nanoparticles

Alzalzalee,

Kassab

2023

IJPS

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Cilnidipine is a dihydropyridine calcium channel blocker used to improve the neurological outcome following subarachnoid hemorrhage. It belongs to BCS class II drugs that have a low oral bioavailability of 13%, thus preparation as nanoparticles would be expected to improve bioavailability. The aim of the study is to prepare Cilnidipine as nanoparticles using different carriers and co-carriers, concentrations, and types. Cilnidipine nanoparticles were prepared by a solvent anti-solvent method using different carriers (Soloplus®, Poloxamer 188, PVA cold) with co-stabilizers (PEG200, glycerol) at different ratios. Based on the obtained results, formula N4, which included Soloplus in a 1:1:1 weight ratio of drug to the polymer to co-stabilizer, exhibited a particle size of 88.89 nm when stirred at 1000 rpm with an injection speed of 1 ml/min. The polydispersity index (PDI) for this formula was measured at 0.2413. Furthermore, formula N4 demonstrated an impressive 92.2% drug content and an entrapment efficiency (EE) of 95.8%, giving 100% release in 30 min.

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Section: Entrapment Efficiency Measurement Of Cld Nanoparticlesmentioning

confidence: 96%

Factors affecting the preparation of Cilnidipine nanoparticles

Alzalzalee,

Kassab

2023

IJPS

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“…To optimize all responses with varying objectives, a response optimizer technique based on the desirability function and a graphical optimization strategy based on the overlay plot was applied [47]. To achieve the optimal balance between the two responses, a composite desirability (D) with values ranging from 0 (unacceptable response value) to 1 (desirable value) was used to optimize both responses simultaneously.…”

Section: Optimization and Validation Of Eco-friendly Degreasermentioning

confidence: 99%

Application of Response Surface Methodology in the Formulation of an Eco-friendly Degreaser using Rhamnolipid Biosurfactant

Muhamad Hissammuddin Shah Zainal Abidin,

Umi Aisah Asli,

Nor Dina Sakaria

et al. 2024

ARASET

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Formulating a bio-based degreaser emulsion can be challenging because it requires maximizing the performance to be as good as a commercial chemical-based product without compromising the cost and effect on the environment. This study aimed to develop an eco-friendly degreaser using natural Rhamnolipid biosurfactant through response surface methodology (RSM), which was then validated and assessed compared to chemical-based commercial products. The Plackett–Burman design (PBD) and Box–Behnken design (BBD) were used to screen and optimize factors for the formulation. From the PBD's result, the amount of Rhamnolipid, with other environmentally friendly ingredients of D-limonene, sodium citrate, and calcium carbonate, were shortlisted as significant factors in the formulation. Next, the BBD optimization study revealed that only rhamnolipid and sodium citrate significantly affected the two-way interaction of the factor on the result of the surface tension and oil displacement test (ODT). In the validation study, the experimental value was very close to the rate predicted by the model for the response surface tension and ODT (24.14 mN/m and 241 mm, respectively). A comparison of the performance with commercial products proved that this formulation was comparable to that commercial product. Overall, this study revealed that the effective eco-friendly degreaser formulation was successfully produced using a minimal amount of rhamnolipid biosurfactant with a response surface methodology as a tool.

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“…Til NCs were prepared using an antisolvent precipitation ultrasonication method [31][32][33]. In brief, crude Til was completely dissolved in DMF:ethanol (1:1).…”

Section: Preparation Of Til Ncsmentioning

confidence: 99%

“…This study aims to develop Til nanocrystals (Til NCs) by an antisolvent precipitation and ultrasonication method [31][32][33]. First, the central composite design (CCD) was utilized to optimize the formulation after a thorough investigation of the formulation's affecting elements was conducted using the single-factor method.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Anti-Inflammatory Activity of Tilianin Based on the Novel Amorphous Nanocrystals

Sun,

Guo,

et al. 2024

Pharmaceuticals

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Tilianin (Til), a flavonoid glycoside, is well-known for its therapeutic promise in treating inflammatory disorders. Its poor water solubility and permeability limit its clinical applicability. In order to overcome these restrictions, an antisolvent precipitation and ultrasonication technique was used to prepare amorphous tilianin nanocrystals (Til NCs). We have adjusted the organic solvents, oil-to-water ratio, stabilizer composition, and ultrasonic power and time by combining single-factor and central composite design (CCD) methodologies. The features of Til NCs were characterized using powder X-ray diffraction (PXRD), scanning calorimetry (DSC), and transmission electron microscopy (TEM). Specifically, the optimized Til NCs were needle-like with a particle size ranging from 90 to 130 nm. PVA (0.3%, w/v) and TPGS (0.08%, w/v) stabilized them well. For at least two months, these Til NCs stayed amorphous and showed an impressive stability at 4 °C and 25 °C. Remarkably, Til NCs dissolved almost 20 times faster in simulated intestinal fluid (SIF) than they did in crude Til. In RAW264.7 cells, Til NCs also showed a better cellular absorption as well as safety and protective qualities. Til NCs were shown to drastically lower reactive oxygen species (ROS), TNF-α, IL-1β, and IL-6 in anti-inflammatory experiments, while increasing IL-10 levels and encouraging M1 macrophages to adopt the anti-inflammatory M2 phenotype. Our results highlight the potential of amorphous Til NCs as a viable approach to improve Til’s anti-inflammatory effectiveness, solubility, and dissolving rate.

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Formulation and optimization of cilnidipine loaded nanosuspension for the enhancement of solubility, dissolution and bioavailability

Cited by 15 publications

References 45 publications

Factors affecting the preparation of Cilnidipine nanoparticles

Factors affecting the preparation of Cilnidipine nanoparticles

Application of Response Surface Methodology in the Formulation of an Eco-friendly Degreaser using Rhamnolipid Biosurfactant

Enhanced Anti-Inflammatory Activity of Tilianin Based on the Novel Amorphous Nanocrystals

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