Effect of Backing Films on the Transdermal Delivery of Donepezil from Patches

Liu, Nannan; Zhang, Yaqiong; Cun, Dongmei; Quan, Peng; Fang, Liang

doi:10.1208/s12249-014-0190-z

Cited by 9 publications

(8 citation statements)

References 22 publications

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“…The purity of DP was determined by HPLC peak area normalization method and higher than 99%. The DSC curve of synthesized product showed a characteristic sharp endothermic peak at 87.26°C which was consistent with its melting point reported in literature [10], which clearly means the successful preparation of DP free base ( Fig.1). …”

Section: Preparation and Identification Of Donepezil Free Basesupporting

confidence: 89%

Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

Guo

Quan

Fang

et al. 2015

Asian Journal of Pharmaceutical Sciences

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Donepezil free base was encapsulated into carboxyl terminal PLGA matrix to obtain high drug loading and encapsulation efficiency. The formulation which sustained release for one week both in vitro and in vivo was designed in order to fulfill various clinical demands. A good correlation between in vitro and in vivo data was obtained. AbstractThe purpose of this study was to develop a PLGA microspheres-based donepezil (DP) formulation which was expected to sustained release DP for one-week with high encapsulation efficiency (EE). DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion-solvent evaporation method. The optimized formulation which avoiding the crushing of microspheres during the preparation process was characterized in terms of particles size, morphology, drug loading and EE, physical state of DP in the matrix and in vitro and in vivo release behavior. DP microspheres were prepared successfully with average diameter around 30 μm, drug loading of 15.92 ± 0.31% and EE up to 78.79 ± 2.56%. Scanning electron microscope image showed it has integrated spherical shape with no drug crystal and porous on its surface.Differential scanning calorimetry and X-ray diffraction results suggested DP was in amorphous state or molecularly dispersed in microspheres. The Tg of PLGA was increased with the addition of DP. The release profile in vitro was characterized with slow but continuous release lasted for about one week and fitted well with First-order model, which suggested the diffusion governing release mechanism. After single-dose administration of DP microspheres via subcutaneous injection in rats, the plasma concentration of DP reached peak concentration at 0.50 d, and then declined gradually, but was still detectable at 15 day. A good correlation between in vitro and in vivo data was obtained.The results suggest the potential use of DP microspheres for treatment of Alzheimer's disease over long periods.

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Section: Preparation and Identification Of Donepezil Free Basesupporting

confidence: 89%

Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

Guo

Quan

Fang

et al. 2015

Asian Journal of Pharmaceutical Sciences

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“…Several recent studies have focused on the development of transdermal forms for administration of donepezil, an anti-Alzheimer drug [60][61][62][63]. In these studies, the permeation of this lipophilic compound (log P > 4) was studied by using different experimental protocols, including skin models, experimental apparatus and formulations.…”

Section: Kinetics Calculationsmentioning

confidence: 99%

Influence of Concentration on Release and Permeation Process of Model Peptide Substance-Corticotropin-From Semisolid Formulations

2020

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The transdermal route of administration of drug substances allows clinicians to obtain a therapeutic effect bypassing the gastrointestinal tract, where the active substance could be inactivated. The hormonal substance used in the study-corticotropin (ACTH)-shows systemic effects. Therefore, the study of the effect of the type of ointment base and drug concentration on the release rate and also permeation rate in in vivo simulated conditions may be a valuable source of information for clinical trials to effectively optimize corticotropin treatment. This goal was achieved by preparation ointment formulation selecting the appropriate ointment base and determining the effect of ACTH concentration on the release and permeation studies of the ACTH. Semi-solid preparations containing ACTH were prepared using Unguator CITO e/s. The release study of ACTH was tested using a modified USP apparatus 2 with Enhancer cells. The permeation study was conducted with vertical Franz cells. Rheograms of hydrogels were made with the use of a universal rotational rheometer. The dependence of the amount of released and permeated hormone on the ointment concentration was found. Based on the test of ACTH release from semi-solid formulations and evaluation of rheological parameters, it was found that glycerol ointment is the most favourable base for ACTH. The ACTH release and permeation process depends on both viscosity and ACTH concentration. The higher the hormone concentration, the higher the amount of released ACTH but it reduces the amount of ACTH penetrating through porcine skin.

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“…Choi and coEvaluation of skin absorption of drugs from topical and transdermal formulations 531 workers (2012) demonstrated a 1-fold reduction in the results of donepezil permeation by using human cadaver skin relative to the results of studies using hairless mouse skin, a skin model with increased permeability. The permeation of donepezil was also studied by Liu et al (2014) who used rabbit abdominal skin and by Subedi and co-workers (2012) who used isolated hairless mouse skin. These authors also achieved satisfactory results by using these skin models; however, the amounts of drug permeated were overestimated in relationship to permeation across normal human skin.…”

Section: In Vitro Evaluation Of the Skin Permeation Of Drugsmentioning

confidence: 99%

“…Thus, selection of the protocol must be performed by using experimental conditions, such as skin model, experimental apparatus, and receptor medium, appropriate for the formulation to be evaluated, and it must be based on the physicochemical properties of the drug, including aqueous solubility and oil-water partition coefficients. Several recent studies have focused on development of transdermal devices for administration of donepezil, an anti-Alzheimer drug Subedi et al, 2012;Saluja et al, 2013;Liu et al, 2014). In these studies, the permeation of this lipophilic compound (log P > 4) was studied by using different experimental protocols, including skin models, experimental apparati, and formulations.…”

mentioning

confidence: 99%

Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

209

135

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The skin barrier function has been attributed to the stratum corneum and represents a major challenge in clinical practice pertaining to cutaneous administration of drugs. Despite this, a large number of bioactive compounds have been successfully administered via cutaneous administration because of advances in the design of topical and transdermal formulations. In vitro and in vivo evaluations of these novel drug delivery systems are necessary to characterize their quality and efficacy. This review covers the most well-known methods for assessing the cutaneous absorption of drugs as an auxiliary tool for pharmaceutical formulation scientists in the design of drug delivery systems. In vitro methods as skin permeation assays using Franz-type diffusion cells, cutaneous retention and tape-stripping methods to study the cutaneous penetration of drugs, and in vivo evaluations as pre-clinical pharmacokinetic studies in animal models are discussed. Alternative approaches to cutaneous microdialysis are also covered. Recent advances in research on skin absorption of drugs and the effect of skin absorption enhancers, as investigated using confocal laser scanning microscopy, Raman confocal microscopy, and attenuated total reflectance Fourier-transform infrared spectroscopy, are reviewed. Uniterms:Skin absorption/effects/study. Skin absorption/topical formulations. Skin absorption/ transdermal formulations. Skin absorptions/enhancers. INTRODUCTIONTopical and transdermal drug delivery systems have shown significant advantages in clinical practice for drug targeting to the action site in the body; this has reduced the systemic side effects. The administration of drugs by through the skin is also performed to achieve controlled or prolonged drug delivery, and this route can be explored as an alternative to the oral route. The oral route shows some limitations for drugs with irregular absorption in the gastrointestinal tract and low bioavailability and for drugs with increased first pass metabolism and short plasma halflife times (Barry, 2001;Wokovich et al., 2006;Prausnitz, Langer, 2009;Alexander et al., 2012).Many drug products applied to the skin surface may penetrate to some extent into the skin layers, where their effects are expected. This is the case for topical formulations for treatment of skin disorders such as acne and cutaneous inflammatory diseases that include dermatitis, erythematous lupus, and psoriasis. On the other hand, transdermal formulations release drugs that permeate through the skin and enter the systemic circulation. Transdermal therapy must ensure that significant concentrations of the drug are absorbed to reach effective plasma concentrations. Permeation of drugs is targeted in some cases to body regions close to the action site, where a regional effect is expected, e.g., in the muscles, blood vessels, and articulations. In this way, the term "cutaneous absorption" is properly used to characterize the sum of the amounts of drug that penetrate and permeate the skin (Barry, 2001;El Maghraby, Barry;Willi...

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Effect of Backing Films on the Transdermal Delivery of Donepezil from Patches

Cited by 9 publications

References 22 publications

Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

Influence of Concentration on Release and Permeation Process of Model Peptide Substance-Corticotropin-From Semisolid Formulations

Evaluation of skin absorption of drugs from topical and transdermal formulations

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