Formulation by design of felodipine loaded liquid and solid self nanoemulsifying drug delivery systems using Box–Behnken design

Verma, Samridhi; Singh, Sandeep Kumar; Verma, Priya Ranjan Prasad; Ahsan, Mohd Neyaz

doi:10.3109/03639045.2013.819884

Cited by 48 publications

(25 citation statements)

References 36 publications

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“…Statistically, the responses were precisely described by the respective models evidenced with the F value of 17.12 (p50.05) and 9.99 for Flux-Span 60 and % EE-Span 60, respectively (Verma et al, 2014). These equations clearly indicated that the Flux-Span 60 and % EE-Span 60 were significantly affected with the concentration of B for flux (p50.0006) and % EE (p50.002), respectively.…”

Section: Preparation Of Elastic Liposomes and Optimizationmentioning

confidence: 60%

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

et al. 2015

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Objective: To prepare and optimize the topical elastic liposome (EL)-loaded carbopol-980 gel of 5-Fluorouracil (5-FU) containing permeation enhancers (azone, propylene glycol (PG) and lauryl alcohol (LA)) and further evaluation for permeation flux of 5-FU, the activation energy and irritation in the rat skin. Methods: EL formulations were prepared using phosphatidylcholine and varied surfactants (Span 60, Span 80 and Tween-80) by rotator evaporation method and optimized by experimental design. In vitro characterizations dictated the EL containing Span 80 (lipid:surfactant ¼ 7:3) (EL3-S80) for further optimization of gel. Different gel formulations (5% w/w) with varying concentration (1-3%) of permeation enhancers were prepared and evaluated for viscosity, spreadability, the 5-FU permeation and deposition. The activation energy using the Franz diffusion cell and the plausible irritation using the Draize test were assessed on the albino rat and rabbit, respectively. Results and discussion: EL3-S80 was selected as an optimized EL owing to maximum desirability (0.99) and enhanced 5-FU flux (187.86 ± 14.1 mg/cm 2 /h). EL3-S80 suspension loaded gels (0.5%) revealed reduced viscosity leading to higher spreadability than blank gel. EL containing 3% azone in gel, EL containing 3% LA in gel and EL containing 3% PG in gel portrayed 187.86 ± 14.1, 117.7 ± 13.4 and 106.7 ± 7.3 mg/cm 2 /h as enhanced 5-FU flux values, respectively as compared to drug solution (8.8 ± 0.76 mg/cm 2 /h). Furthermore, reduced value of activation energy (2.63-folds) and the non-irritancy of gel could be effective and safe. Conclusion: ELA-3 gel formulation could be used as an effective and economic gel in cutaneous cancer and skin-related keratoses.

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Section: Preparation Of Elastic Liposomes and Optimizationmentioning

confidence: 60%

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

et al. 2015

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“…Zeta potential was determined without dilution using a 4.0 mW He-Ne red laser (633 nm) to measure the surface charge from −120 to 120 mV. 20 The pH values of all formulations were determined using an HI 9321 pH meter (an electrode meter) (Hanna Instruments, Ann Arbor, MI, USA).…”

Section: Characterization Of Nanoemulsionsmentioning

confidence: 99%

<p>Novel Approach for Transdermal Delivery of Rifampicin to Induce Synergistic Antimycobacterial Effects Against Cutaneous and Systemic Tuberculosis Using a Cationic Nanoemulsion Gel</p>

Hussain¹,

Altamimi²,

Alshehri³

et al. 2020

IJN

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This study demonstrated improved transdermal delivery of rifampicin-loaded cationic nanoemulsion gel to treat systemic and cutaneous tuberculosis using capmul, labrasol, and acconon, which exert anti-Mycobacterium activities. This approach enhanced drug permeation across the skin, increased therapeutic efficacy, and reduced dose-related side effects. Methods: Design Expert ® was used to optimize formulations (S mix ratio and capmul as independent factors), which were prepared using a slow spontaneous titration method. The optimized nanoemulsion was incorporated into carbopol gel to allow for topical application and comparative assessments. Nanoemulsions and gels were evaluated for size, size distribution, shape, zeta potential, percent spread, viscosity, in vitro hemolysis, in vitro release, and ex vivo skin permeation and deposition. A mechanistic evaluation was performed using scanning electron microscopy. Furthermore, in vivo pharmacokinetic and irritation studies were performed. Results: The optimized cationic nanoemulsion (OCNE-1) was characterized by small particle size (≤100 nm), had optimal viscosity, percent spread, zeta potential, and percent drug release, and was hemocompatible. The OCNE-1T gel exhibited higher permeation flux (51.32 ± 0.5 µg/cm 2 hr), permeation coefficient (2.566 ± 0.08 cm/hr), drug deposition (994.404 µg/cm 2), and enhancement ratio (7.16) than those of the OCNE-1 nanoemulsion or drug solution. Scanning electron microscopy was used to characterize the mechanism of enhanced permeation. An In vivo study showed that the C max and area under the curve following transdermal application were 4.34-and 4.74-fold higher than those following oral administration. Conclusion: Transdermal delivery of rifampicin could be a promising alternative to conventional approaches to treat systemic and local tuberculosis, and other bacterial infections.

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“…The optimization design of CUR-CNLC and the data were analyzed by Design-Expert software (8.06 version, Stat Ease, Inc., Minneapolis, U.S.) [31]. The results were presented as the mean ± standard deviation (SD).…”

Section: Discussionmentioning

confidence: 99%

A novel cationic nanostructured lipid carrier for improvement of ocular bioavailability: Design, optimization, in vitro and in vivo evaluation

Wang

Sun

et al. 2016

Journal of Drug Delivery Science and Technology

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The objective of this study was to prepare, optimize and evaluate a novel cationic nanostructured lipid carrier (CNLC) system, which can enhance the ophthalmic bioavailability of curcumin (CUR). CUR-loaded CNLC (CUR-CNLC) was prepared using a film-ultrasonic technique. A three-level Box-Behnken design was applied for optimization. The physicochemical properties, in vitro release and corneal permeation of the delivery method were evaluated. Preocular retention capacity study was conducted using a non-invasive fluorescence imaging system. Finally, a pharmacokinetic study in the aqueous humor was performed using a microdialysis technique. The optimal formulation had a mean particle size of 158.1 nm with a homogeneous distribution, a positive surface charge of 36.5 mV, a high entrapment efficiency of 99.12% and drug loading of 1.677%. Transmission electron microscope (TEM) morphology depicted a spherical morphology, and differential scanning calorimetry (DSC) indicated an imperfect crystalline lattice for the formulation. The CUR-CNLC formulation exhibited a sustained drug release and a 1.25-fold increase in in vitro corneal permeation (P<0.05). The results from in vivo studies indicated the formulation had a high tolerance and a prolonged drug retention capacity in ocular tissues. A pharmacokinetic study of rabbit aqueous humors demonstrated a 2.36-fold increase in ocular bioavailability compared to a CUR solution (CUR-SOL, P<0.01). The amphipathic octadecyl-quaternized carboxymethyl chitosan (QACMC) was used as a novel cationic material to prolong the residence time and improve the ocular bioavailability. Therefore, CNLC system is a promising approach for ocular delivery of CUR.

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Formulation by design of felodipine loaded liquid and solid self nanoemulsifying drug delivery systems using Box–Behnken design

Abstract: This study indicates that owing to nanosize, SNEDDS and S-SNEDDS of FLD have potential to enhance its absorption and may serve an efficient oral delivery.

Cited by 48 publications

References 36 publications

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

<p>Novel Approach for Transdermal Delivery of Rifampicin to Induce Synergistic Antimycobacterial Effects Against Cutaneous and Systemic Tuberculosis Using a Cationic Nanoemulsion Gel</p>

A novel cationic nanostructured lipid carrier for improvement of ocular bioavailability: Design, optimization, in vitro and in vivo evaluation

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