Preparation of celecoxib solid dispersions for dermal application: in vitro characterization and skin irritation test

Soliman, Sara M.; Malak, Nevine S. Abdel; El‐Gazayerly, Omaima N.; Rehim, A.A. Abdel

doi:10.1016/s1773-2247(11)50082-6

Cited by 22 publications

(22 citation statements)

References 33 publications

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“…Firstly, we demonstrated that COX-2 and TGF Beta-1 showed similar cellular profiles as both were expressed mainly by the infiltrating inflammatory cells in the wound area, this was in line with other studies [52][53][54][55], however, we endorsed our finding by showing for the first time actual colocalization of Cox-2 and TGF Beta-1 on the cellular level in the wound area. Secondarily, demonstrating that both mediators showed a similar pattern of expression in the wound, where COX-2 upregulation and downregulation was associated with a concomitant similar change in TGF Beta-1, this was in line with other studies in different animal models of inflammation [61][62][63][64][65][66][67][68][69][70]. Thirdly, we endorsed this COX-2 and TGF Beta-1 coordinated relation results further by a correlation studies that showed for the first time a strong correlation between COX-2 and TGF Beta-1 in dermal wounds.…”

Section: Discussionsupporting

confidence: 88%

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Inhibition of Wound TGF Beta-1 by Celecoxib: A Possible Therapeutic Route for Scar Free Wound

El-Aleem¹,

Jude²

2017

J Cytol Histol

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Background: Wound healing is a highly ordered dynamic process associated with inflammation at early stages and with permanent scarring at late stages. Scars could be disfiguring and could advance to be hypertrophic or keloid scars, this would have a strong physical and psychological impact on the patients afterward. The role of inflammatory mediators which could be pro-or anti-inflammatory, pro-or -anti fibrotic was the focus of wound healing research for decades and the balance between them is the key factor determining the outcome of healing.

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Section: Discussionsupporting

confidence: 88%

“…Celecoxib is a NSAID that selectively inhibits COX-2 with anti-inflammatory effect but lesser toxicity than other NSAIDs [66]. We have shown that inhibition of wound COX-2 resulted in inhibition of wound TGF Beta-1 and improvement in wound repair progression as demonstrated by reducing inflammation and early wound closure.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of Wound TGF Beta-1 by Celecoxib: A Possible Therapeutic Route for Scar Free Wound

El-Aleem¹,

Jude²

2017

J Cytol Histol

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“…Usually, the skin irritation test was performed to check suitable concentrations of components employed for microemulsion preparation. This test was conducted to find out the optimized microemulsion localized reaction on the skin (49). Skin erythema index represents the optimized formulations skin irritation (50).…”

Section: Skin Irritation Studymentioning

confidence: 99%

Microemulsion and microemulsion based gel of Zaleplon for transdermal delivery: Preparation, optimization, and evaluation

Naeem¹

2019

Acta Poloniae Pharmaceutica - Drug Research

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Zaleplon (pyrazolopyrimidine hypnotic drug) prescribed for the management of short term insomnia (1-2). It exhibits ideal characteristics like having low molecular weight of 305.54, ideal logarithmic partition coefficient of log octanol/water: 1.23, little dose of 1 mg to 10 mg, poor oral bioavailability of 30.6 ± 10.2%, and half-life of 1.05 ± 0.13 h for preparing transdermal delivery (3). Despite, the drug comes across broad first-pass hepatic metabolism following oral absorption which results in only 30% bioavailability (4). Additionally, Zaleplon shows very little water solubility which owes to absorption is found to be dissolution rate-limited that concludes delayed and sustained onset of action (5-6). This dispute can be resolved by using microemulsion, a successful vehicle that potentially and optimally increases drug solubility and permeation on skin. BCS II is an appropriate class of drugs formulated in microemulsion to enhance drug solubility and permeability (7-9).

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“…This assembly was placed at the bottom of the dissolution vessel containing 500 ml of 30% methanolic solution (v/v) with constant speed (100 rpm) at 37 ± 0.5 C. Methanol was added to maintain the sink conditions during the release study due to the extreme poor solubility of lacidipine in water (Fang et al, 2001;El-Laithy et al, 2011). At predetermined time intervals (0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 24 h), aliquots of 5 ml of the release medium were withdrawn and replaced with equal volume of fresh medium to maintain a constant volume (Soliman et al, 2011). The concentration of lacidipine of the collected samples was determined spectrophotometrically at the predetermined l max of 286 nm.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

“…The mean erythemal or edema scores were recorded (ranging from 0 to 4) according to Draize (Draize et al, 1944), where 0 means no erythema or edema, 1 slight erythema or edema, 2 moderate erythema or edema, 3 moderate to severe erythema or edema, and 4 severe erythema or edema. The primary irritancy index (PII) was calculated by adding the edema and the erythema scores (Soliman et al, 2010(Soliman et al, , 2011.…”

Section: Skin Irritation Testmentioning

confidence: 99%

Novel non-ionic surfactant proniosomes for transdermal delivery of lacidipine: optimization using 2³factorial design andin vivoevaluation in rabbits

et al. 2016

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Context: Proniosomes offer a versatile vesicle drug delivery concept with potential for delivery of drugs via transdermal route. Objectives: To develop proniosomal gel using cremophor RH 40 as non-ionic surfactant containing the antihypertensive drug lacidipine for transdermal delivery so as to avoid its extensive first pass metabolism and to improve its permeation through the skin. Materials and methods: Proniosomes containing 1% lacidipine were prepared by the coacervation phase separation method, characterized, and optimized using a 2 3 full factorial design to define the optimum conditions to produce proniosomes with high entrapment efficiency, minimal vesicle size, and high-percentage release efficiency. The amount of cholesterol (X 1 ), the amount of soya lecithin (X 2 ), and the amount of cremophor RH 40 (X 3 ) were selected as three independent variables. Results and discussion: The system F4 was found to fulfill the maximum requisite of an optimum system because it had minimum vesicle size, maximum EE, maximum release efficiency, and maximum desirability. The optimized system (F4) was then converted to proniosomal gel using carbopol 940 (1% w/w). In vitro permeation through excised rabbit skin study revealed higher flux (6.48 ± 0.45) for lacidipine from the optimized proniosomal gel when compared with the corresponding emulgel (3.04 ± 0.13) mg/cm 2 /h. The optimized formulation was evaluated for its bioavailability compared with commercial product. Statistical analysis revealed significant increase in AUC (0 À a) 464.17 ± 113.15 ng h/ml compared with 209.02 ± 47.35 ng h/ml for commercial tablet. Skin irritancy and histopathological investigation of rat skin revealed its safety. Conclusions: Cremophor RH 40 proniosomal gel could be considered as very promising nanocarriers for transdermal delivery of lacidipine. KeywordsBioavailability study, 2 3 full factorial design, lacidipine, proniosomal gel transdermal delivery History

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Preparation of celecoxib solid dispersions for dermal application: in vitro characterization and skin irritation test

Cited by 22 publications

References 33 publications

Inhibition of Wound TGF Beta-1 by Celecoxib: A Possible Therapeutic Route for Scar Free Wound

Inhibition of Wound TGF Beta-1 by Celecoxib: A Possible Therapeutic Route for Scar Free Wound

Microemulsion and microemulsion based gel of Zaleplon for transdermal delivery: Preparation, optimization, and evaluation

Novel non-ionic surfactant proniosomes for transdermal delivery of lacidipine: optimization using 2³factorial design andin vivoevaluation in rabbits

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Preparation of celecoxib solid dispersions for dermal application: in vitro characterization and skin irritation test

Cited by 22 publications

References 33 publications

Inhibition of Wound TGF Beta-1 by Celecoxib: A Possible Therapeutic Route for Scar Free Wound

Inhibition of Wound TGF Beta-1 by Celecoxib: A Possible Therapeutic Route for Scar Free Wound

Microemulsion and microemulsion based gel of Zaleplon for transdermal delivery: Preparation, optimization, and evaluation

Novel non-ionic surfactant proniosomes for transdermal delivery of lacidipine: optimization using 23factorial design andin vivoevaluation in rabbits

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Product

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Novel non-ionic surfactant proniosomes for transdermal delivery of lacidipine: optimization using 2³factorial design andin vivoevaluation in rabbits