Formulation of Hydrophilic Non-Aqueous Gel: Drug Stability in Different Solvents and Rheological Behavior of Gel Matrices

Chow, Keat Theng; Chan, Lai Wah; Heng, Paul Wan Sia

doi:10.1007/s11095-007-9457-3

Cited by 33 publications

(29 citation statements)

References 38 publications

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“…Incorporation of niosomes in semisolid gel forms a colloidal network that aligns itself in the direction of applied shear showing pseudoplastic behavior (a shear thinning system showing decrease in viscosity on application of shear stress) which facilitates its topical application (19)(20)(21). Lor-Nio gel had better spreadability over plain Carbopol gel.…”

Section: Discussionmentioning

confidence: 99%

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Niosomal Gel of Lornoxicam for Topical Delivery: In vitro Assessment and Pharmacodynamic Activity

2013

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Abstract. Lornoxicam is a potent oxicam class of non steroidal anti-inflammatory agent, prescribed for mild to moderate pain and inflammation. Niosomal gel of lornoxicam was developed for topical application. Lornoxicam niosomes (Lor-Nio) were fabricated by thin film hydration technique. Bilayer composition of niosomal vesicles was optimized. Lor-Nio dispersion was characterized by DSC, XRD, and FT-IR. Morphological evaluation was performed by scanning electron microscopy (SEM). Lor-Nio dispersion was incorporated into a gel using 2% w/w Carbopol 980 NF. Rheological and texture properties of LorNio gel formulation showed suitability of the gel for topical application. The developed formulation was evaluated for in vitro skin permeation and skin deposition studies, occlusivity test and skin irritation studies. Pharmacodynamic activity of the Lor-Nio gel was performed by carragenan-induced rat paw model. Optimized Lor-Nio comprised of Span 60 and cholesterol in a molar ratio of 3:1 with 30 μM dicetyl palmitate as a stabilizer. It had particle size of 1.125±0.212 μm (d 90 ), with entrapment efficiency of 52.38± 2.1%. DSC, XRD, and IR studies showed inclusion of Lor into niosomal vesicles. SEM studies showed spherical closed vesicular structure with particles in nanometer range. The in vitro skin permeation studies showed significant improvement in skin permeation and skin deposition for Lor-Nio gel (31.41±2.24 μg/ cm 2 , 30.079±1.2 μg/cm 2 ) over plain lornoxicam gel (7.37±1.27 μg/cm 2 , 6.6±2.52 μg/cm 2 ). The Lor-Nio gel formulation showed enhanced anti-inflammatory activity by exhibiting mean edema inhibition (87.69± 1.43%) which was significantly more than the plain lornoxicam gel (53.84±2.21%).

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Section: Discussionmentioning

confidence: 99%

“…Dynamic shear strain ranging from 0.1 to 100 S −1 was applied to the sample and the shear stress and the viscosity expended by the sample by imposed shear strain was measured. The measurements were performed at isothermal condition of 37°C (19)(20)(21).…”

Section: Characterization Of Optimized Lor-nio Dispersionmentioning

confidence: 99%

Niosomal Gel of Lornoxicam for Topical Delivery: In vitro Assessment and Pharmacodynamic Activity

2013

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“…This phase angle shift which is the time shift between the strain and stress amplitudes (Δt) was measured as the damping factor which is tangent of the phase angle shift. Various parameters like loss modulus (G″), storage modulus (G′), and complex viscosity (ŋ*) were measured in order to measure the viscous and elastic behavior of the gels (26,27).…”

Section: Rheological Evaluation Of Trb Nlhmentioning

confidence: 99%

Nanolipidgel for Enhanced Skin Deposition and Improved Antifungal Activity

Wavikar

Vavia

2012

AAPS PharmSciTech

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Abstract. The purpose of the research was to prepare and evaluate a topical nanolipidgel (NLH) of terbinafine hydrochloride (TRB), an antimycotic agent, for enhanced skin deposition and improved antifungal activity. Topical solid lipid nanoparticles (SLN) based nanolipidgel was formulated and evaluated. TRB-loaded SLNs were formulated by high-pressure homogenization technique. The stable TRB SLN dispersion was incorporated into a gel using 1% Carbopol 980 NF. Rheological evaluation and texture analysis of the TRB NLH was carried out. Skin permeation, skin deposition, antifungal activity, and occlusivity studies of the nanolipidgel formulation were carried out. The safety of the TRB NLH gel was evaluated using acute skin irritation test on New Zealand White rabbits. The SLN dispersion containing 10% of glyceryl monostearate, 3% of Tween 80, and 1% Plurol Oleique was the most stable. The optimized TRB SLN had a particle size and zeta potential value of 148.6 ± 0.305 nm and −20.4 ±1.2 mV, respectively. TRB NLH had excellent rheological and texture properties to facilitate its topical application. TRB NLH showed increased skin deposition of the drug over plain (3-fold) and marketed TRB formulation (2-fold). TRB NLH had significantly enhanced antifungal activity against Candida albicans. TRB NLH showed efficient occlusivity and was non-irritant to the rabbit skin with no signs of erythema or edema. Solid lipid nanoparticles-based topical nanolipidgel of terbinafine can be an efficient, industrially scalable, and cost-effective alternative to the existing conventional formulations.KEY WORDS: in vitro antifungal activity; rheological analysis of gel; solid lipid nanoparticles; terbinafine; texture analysis of gel.

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“…Nonaqueous gel formulations have been a useful vehicle for moisture-sensitive drugs for topical and transdermal application (20)(21)(22)(23)(24). Critical components for the successful development of a semisolid product for topical and transdermal applications include the stability of the active pharmaceutical ingredient (API) in the delivery matrix, product uniformity, and the release profile of API from the delivery matrix.…”

Section: Discussionmentioning

confidence: 99%

“…The major degradation pathway involved with moisture-sensitive drugs is hydrolysis followed by secondary degradation reactions such as polymerization and isomerization (19). In contrast to extensive research on traditional semisolid dosage forms such as creams, ointments, and hydrogels, there are far fewer reports on the development of nonaqueous gel matrices intended for topical and transdermal drug delivery (20)(21)(22)(23)(24). Ethyl cellulose is frequently used as a gelling agent for nonaqueous gel vehicles.…”

Section: Introductionmentioning

confidence: 99%

Nonaqueous Gel for the Transdermal Delivery of a DTPA Penta-ethyl Ester Prodrug

Zhang

Sadgrove

Sueda

et al. 2013

AAPS J

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Abstract. Diethylenetriamine pentaacetic acid penta-ethyl ester, designated as C2E5, was successfully incorporated into a nonaqueous gel for transdermal delivery. The thermal and rheological properties of a formulation containing 40% C2E5, 20% ethyl cellulose, and 40% Miglyol 840® prepared using the solvent evaporation method demonstrated that the gel had acceptable content uniformity and flow properties. In vitro studies showed that C2E5 was steadily released from the gel at a rate suitable for transdermal delivery. Topical application of the gel at a 200 mg C2E5/kg dose level in rats achieved significantly higher plasma exposures of several active metabolites compared with neat C2E5 oil at the same dose level. The results suggest that transdermal delivery of a chelator prodrug is an effective radionuclide decorporation strategy by delivering chelators to the circulation with a pharmacokinetic profile that is more consistent with the biokinetic profile of transuranic elements in contaminated individuals.

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Formulation of Hydrophilic Non-Aqueous Gel: Drug Stability in Different Solvents and Rheological Behavior of Gel Matrices

Cited by 33 publications

References 38 publications

Niosomal Gel of Lornoxicam for Topical Delivery: In vitro Assessment and Pharmacodynamic Activity

Niosomal Gel of Lornoxicam for Topical Delivery: In vitro Assessment and Pharmacodynamic Activity

Nanolipidgel for Enhanced Skin Deposition and Improved Antifungal Activity

Nonaqueous Gel for the Transdermal Delivery of a DTPA Penta-ethyl Ester Prodrug

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