Transdermal Delivery of Gabapentin: Effect of Cosolvent and Microemulsion on Permeation through the Rat Skin

Mbah, Chika J; Nnadi, Charles Okeke

doi:10.4236/pp.2014.55057

Cited by 6 publications

(12 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Furthermore, complex formulations have also been investigated for the delivery of highly hydrophilic molecules. For example, Steluti et al delivered 5-aminolevulinic acid from propylene glycol solutions containing glycerol monooleate [ 10 ], whilst Mbah and Nnadi successfully delivered gabapentin from both water-in-oil and oil-in-water microemulsions [ 11 ].…”

Section: Introductionmentioning

confidence: 99%

“…When topical products are formulated, a critical factor to consider is the ability of the drug molecule to enter and cross the skin, or other biological barrier, whether intended for local or systemic delivery. Typically, skin permeation studies employ a Franz-type diffusion cell assembly to investigate the potential of formulations to deliver substances through skin in vitro [ 10 , 11 , 12 , 13 ]. A variety of model permeation barriers are employed in such diffusion studies, ranging from synthetic membranes to biological membranes and tissues derived from animal and human skin.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Development and Evaluation of Topical Gabapentin Formulations

et al. 2017

View full text Add to dashboard Cite

Topical delivery of gabapentin is desirable to treat peripheral neuropathic pain conditions whilst avoiding systemic side effects. To date, reports of topical gabapentin delivery in vitro have been variable and dependent on the skin model employed, primarily involving rodent and porcine models. In this study a variety of topical gabapentin formulations were investigated, including Carbopol® hydrogels containing various permeation enhancers, and a range of proprietary bases including a compounded Lipoderm® formulation; furthermore microneedle facilitated delivery was used as a positive control. Critically, permeation of gabapentin across a human epidermal membrane in vitro was assessed using Franz-type diffusion cells. Subsequently this data was contextualised within the wider scope of the literature. Although reports of topical gabapentin delivery have been shown to vary, largely dependent upon the skin model used, this study demonstrated that 6% (w/w) gabapentin 0.75% (w/w) Carbopol® hydrogels containing 5% (w/w) DMSO or 70% (w/w) ethanol and a compounded 10% (w/w) gabapentin Lipoderm® formulation were able to facilitate permeation of the molecule across human skin. Further pre-clinical and clinical studies are required to investigate the topical delivery performance and pharmacodynamic actions of prospective formulations.

show abstract

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of Topical Gabapentin Formulations

et al. 2017

View full text Add to dashboard Cite

show abstract

“…For a drug, which doesn"t possess a favourable o/w partition coefficient this route cannot be used. From one site to another on the same person, from person to person and with age the barrier functions of the skin changes which hinders transdermal drug penetration 7,8 .…”

Section: Limitations Of Transdermal Drug Deliverymentioning

confidence: 99%

Untitled

2019

IJPSR

View full text Add to dashboard Cite

Transdermal drug delivery system (TDDS) provides a leading edge over injectables and oral routes by increasing patient compliance and avoiding the first-pass metabolism respectively. Transdermal delivery not only provides controlled, constant administration of the drug, but also allows continuous input of drugs with short biological half-lives and eliminates pulsed entry into the systemic circulation, which often causes undesirable side effects. The oral route of transdermal drug delivery enables avoidance in gastrointestinal absorption. One of the greatest innovations of novel drug delivery in transdermal patch skin adhesion is the most important functional properties for a TDDS. Poor adhesion results in improper dosing of patients and potential accidental dosing of patients, who may pick up fallen patches. The adhesive of the TDDS is critical to the safety, efficacy, and quality of the product. Drug therapy may be terminated rapidly by the removal of the application from the surface of the skin. This article provides a framework for scientific work to improve transdermal adhesive performance and provides an overview of types of transdermal, their anatomy, and the role of adhesion, the possible adhesion failure modes and how adhesion can be measured. Topical administration of therapeutic agents offers many advantages over conventional oral and invasive methods of drug delivery. FDA reports on the lack of adhesion of transdermal system products are presented. Pros and cons of in-vitro techniques, such as peel adhesion, tack and shear strength in-vivo techniques used to evaluate adhesive properties are discussed.

show abstract

“…The epidermis was prepared from the full thickness skin by heat separation technique 23 . It involved soaking entire abdominal skin in water at 60 ºC for 1 min.…”

Section: Preparation Of Epidermismentioning

confidence: 99%

Untitled

2018

IJPSR

View full text Add to dashboard Cite

The objective of the study was to investigate the effect of microemulsion on in-vitro skin permeation, percutaneous absorption of Irbesartan and to postulate probable mechanism of skin permeation. Microemulsion was prepared by aqueous phase titration method. Pseudoternary phase diagrams were constructed for the microemulsions. Thermodynamic stability study was carried out on selected microemulsions. Characterization of selected Irbesartan-loaded microemulsions was done by droplet size and polydispersity index determination. Physicochemical properties of Irbesartan-loaded microemulsions were determined using reported procedures. In-vitro skin permeation was determined using Franz cell. Skin permeation mechanism was assessed by Fourier Transform Infra-Red spectra analysis, Differential Scanning Calorimetry and activation energy measurement. A non-compartmental pharmacokinetic study was carried out to estimate the percutaneous absorption through the rat skin. The particle size and polydispersity index of the spherically shaped microemulsions were in the range of 83-86 nm and 0.270-0.290 respectively. In-vitro skin permeation study gave the permeability coefficient and steady state flux of Irbesartan to be 3.52 (×10-3) cm/h and 17.59 ± 0.38 µg/cm 2 /h for oil-in-water (O/W); 6.63 (×10-3) cm/h and 33.16 ± 0.33 µg/cm 2 /h for water-in-oil (W/O) respectively. Compared with the Irbesartan suspensions, pharmacokinetics of Irbesartan-loaded microemulsions in Wistar rats indicated higher plasma drug concentrations and larger area under the curve. The pharmacokinetic and in-vitro studies suggest that microemulsion could be an effective transdermal drug delivery system to improve bioavailability of Irbesartan. Disruption of lipid bilayer, protein denaturation and skin hydration are considered to be the probable skin permeation mechanism.

show abstract

Transdermal Delivery of Gabapentin: Effect of Cosolvent and Microemulsion on Permeation through the Rat Skin

Cited by 6 publications

References 27 publications

Development and Evaluation of Topical Gabapentin Formulations

Development and Evaluation of Topical Gabapentin Formulations

Untitled

Untitled

Contact Info

Product

Resources

About