Response surface optimization of biocompatible elastic nanovesicles loaded with rosuvastatin calcium: enhanced bioavailability and anticancer efficacy

Elsayed, Ibrahim; El-Dahmy, Rania Moataz; El-Emam, Soad Z.; Elshafeey, Ahmed Hassen; Gawad, Nabaweya Abdelaziz Abd El; El‐Gazayerly, Omaima N.

doi:10.1007/s13346-020-00761-0

Cited by 24 publications

(14 citation statements)

References 105 publications

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“…This could be a result of aggregation of bilosomes due to the high level of utilized lipids. Our findings are similar to those reported by Elsayed et al [32] and Hao and Li [36].…”

Section: Effect Of Variables On Vssupporting

confidence: 93%

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Clove Oil Endorsed Transdermal Flux of Dronedarone Hydrochloride Loaded Bilosomal Nanogel: Factorial Design, In vitro Evaluation and Ex vivo Permeation

2022

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The goal of this study was to develop a bilosomal gel formulation to enhance transdermal permeability of dronedarone hyrdrochloride (DRN) which suffers from poor oral absorption and limited bioavailability. To overcome this obstacle, bilosomes were successfully prepared using 23 full-factorial design. Span®40, cholesterol, sodium deoxycholate (bile salt), clove oil (permeability enhancer), and either Tween® 60 or Tween® 80 (edge activator) were used in bilosome preparation by ethanol injection method. In this design, independent variables were X1, edge activator type; X2, edge activator amount (mg); and X3, permeability enhancer concentration (% w/v). Optimal formula (B2) of the highest desirability of (0.776) demonstrated minimum vesicle size (VS) of 312.4 ± 24.42 nm, maximum absolute value of zeta potential (ZP) − 36.17 ± 2.57 mV, maximum entrapment efficiency (EE %) of 80.95 ± 3.01%, maximum deformability Index (DI) of 8.24 ± 1.26 g and maximum drug flux after 12 h (J12) of 21.23 ± 1.54 µg/cm2 h upon ex vivo permeation study. After 12 h, 70.29 ± 6.46% of DRN was released from B2. TEM identification of B2 showed spherical shaped nanosized vesicles which were physically stable for 3 months at different temperatures. B2 was incorporated into carboxymethylcellulose gel base for easiness of dermal application. B2 gel demonstrated good physical properties, non-Newtonian psuedoplastic flow, and enhanced release (57.0 ± 8.68% of DRN compared to only 13.3 ± 1.2% released from drug suspension after 12 h) and enhanced skin permeation. Graphical abstract

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“…This could be a result of aggregation of bilosomes due to the high level of utilized lipids. Our findings are similar to those reported by Elsayed et al [32] and Hao and Li [36].…”

Section: Effect Of Variables On Vssupporting

confidence: 93%

“…PDI is preferred to be less than 0.3 but values less than 0.7 are still acceptable because different size distribution algorithms work with data that fall between PDI range (0.05-0.7) [31]. If the value goes beyond 0.7, the sample cannot be analyzed by dynamic light scattering method [32].…”

Section: Effect Of Variables On Vsmentioning

confidence: 99%

Clove Oil Endorsed Transdermal Flux of Dronedarone Hydrochloride Loaded Bilosomal Nanogel: Factorial Design, In vitro Evaluation and Ex vivo Permeation

2022

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“…Then, 4 mL of sample was withdrawn at 2, 4, 6, 8, 10, 15, 30, 45, and 60 min time intervals. Then, 4 mL of fresh phosphate buffer was replenished to keep a constant medium volume [30,31]. Finally, PX concentration was detected spectrophotometrically in each sample at λ max 294.3 nm [3].…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

“…To identify the optimal OFDF, it was nearly impossible to fulfill all the desired responses at the same time, because the optimum condition fulfilled for one response could adversely affect other responses [22]. However, the desirability function combined all the desired responses in one variable, in order to determine the optimum levels of the examined factors [31]. Figure 3c shows that the highest desirability value was 0.659 for the optimized PX OFDF (F1) containing pectin polymer with a concentration of 1% w/v and glycerol as a plasticizer.…”

Section: Selection Of the Optimized Ofdf Loaded With Px Nanosuspensionmentioning

confidence: 99%

“…These results could also be attributed to the incorporation of tween 80 into the optimized film. Whereby, this surfactant provided an elastic effect that loosened or fluidized the mucosal membrane lipid bilayer and made the drug capable of squeezing into deeper layers of the biological membrane, leading to the enhancement of drug permeability through the buccal mucosa [31]. Regarding the mechanism of PX transport across the buccal mucosal membrane, the uptake process was concentration-dependent, via simple diffusion [67].…”

Section: Stability Studymentioning

confidence: 99%

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Formulation and Development of Oral Fast-Dissolving Films Loaded with Nanosuspension to Augment Paroxetine Bioavailability: In Vitro Characterization, Ex Vivo Permeation, and Pharmacokinetic Evaluation in Healthy Human Volunteers

Elshafeey

El-Dahmy

2021

Pharmaceutics

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Paroxetine (PX) is the most potent serotonin reuptake inhibitor utilized in depression and anxiety treatment. It has drawbacks, such as having a very bitter taste, low water solubility, and undergoing extensive first pass metabolism, leading to poor oral bioavailability (<50%). This work aimed to develop and optimize palatable oral fast-dissolving films (OFDFs) loaded with a paroxetine nanosuspension. A PX nanosuspension was prepared to increase the PX solubility and permeability via the buccal mucosa. The OFDFs could increase PX bioavailability due to their rapid dissolution in saliva, without needing water, and the rapid absorption of the loaded drug through the buccal mucosa, thus decreasing the PX metabolism in the liver. OFDFs also offer better convenience to patients with mental illness, as well as pediatric, elderly, and developmentally disabled patients. The PX nanosuspension was characterized by particle size, poly dispersity index, and zeta potential. Twelve OFDFs were formulated using a solvent casting technique. A 22 × 31 full factorial design was applied to choose the optimized OFDF, utilizing Design-Expert® software (Stat-Ease Inc., Minneapolis, MN, USA). The optimized OFDF (F1) had a 3.89 ± 0.19 Mpa tensile strength, 53.08 ± 1.28% elongation%, 8.12 ± 0.13 MPa Young’s modulus, 17.09 ± 1.30 s disintegration time, and 96.02 ± 3.46% PX dissolved after 10 min. This optimized OFDF was subjected to in vitro dissolution, ex vivo permeation, stability, and palatability studies. The permeation study, using chicken buccal pouch, revealed increased drug permeation from the optimized OFDF; with a more than three-fold increase in permeation over the pure drug. The relative bioavailability of the optimized OFDF in comparison with the market tablet was estimated clinically in healthy human volunteers and was found to be 178.43%. These findings confirmed the success of the OFDFs loaded with PX nanosuspension for increasing PX bioavailability.

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Pharmacokinetics and Pharmacodynamics of Nanocarriers and Novel Drug Delivery Systems

Gharat,

Momin,

Khan

2024

Pharmacokinetics and Pharmacodynamics of Novel Drug Delivery Systems: From Basic Concepts to Applications

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Response surface optimization of biocompatible elastic nanovesicles loaded with rosuvastatin calcium: enhanced bioavailability and anticancer efficacy

Cited by 24 publications

References 105 publications

Clove Oil Endorsed Transdermal Flux of Dronedarone Hydrochloride Loaded Bilosomal Nanogel: Factorial Design, In vitro Evaluation and Ex vivo Permeation

Clove Oil Endorsed Transdermal Flux of Dronedarone Hydrochloride Loaded Bilosomal Nanogel: Factorial Design, In vitro Evaluation and Ex vivo Permeation

Formulation and Development of Oral Fast-Dissolving Films Loaded with Nanosuspension to Augment Paroxetine Bioavailability: In Vitro Characterization, Ex Vivo Permeation, and Pharmacokinetic Evaluation in Healthy Human Volunteers

Pharmacokinetics and Pharmacodynamics of Nanocarriers and Novel Drug Delivery Systems

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