Transdermal insulin delivery with microwave and fatty acids as permeation enhancers

Harjoh, Nurulaini; Wong, Tin Wui; Caramella, Carla

doi:10.1016/j.ijpharm.2020.119416

Cited by 22 publications

(14 citation statements)

References 42 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Rowat and colleagues discovered that oleic acid can cause phase separation in a simulated stratum corneum membrane containing bovine brain ceramide, cholesterol, and palmitic acid, which changes the structure and permeability of the stratum corneum [ 137 ]. Since oleic acid increases skin permeation by stimulating epidermal lipid bilayer fluidization and corneocyte shrinkage via keratin condensation [ 138 ], resulting in the enlargement of aqueous pores for transdermal drug delivery [ 138 ], oleic acid-containing vesicles are expected to enable hydrophilic drug transportation through the skin. In addition, the surface charge of the PRO–CTS–UFAs was the essential aspect in deciding how the CTS may improve skin drug delivery.…”

Section: Resultsmentioning

confidence: 99%

Sustainable Release of Propranolol Hydrochloride Laden with Biconjugated-Ufasomes Chitosan Hydrogel Attenuates Cisplatin-Induced Sciatic Nerve Damage in In Vitro/In Vivo Evaluation

et al. 2022

View full text Add to dashboard Cite

Peripheral nerve injuries significantly impact patients’ quality of life and poor functional recovery. Chitosan–ufasomes (CTS–UFAs) exhibit biomimetic features, making them a viable choice for developing novel transdermal delivery for neural repair. This study aimed to investigate the role of CTS–UFAs loaded with the propranolol HCl (PRO) as a model drug in enhancing sciatica in cisplatin-induced sciatic nerve damage in rats. Hence, PRO–UFAs were primed, embedding either span 20 or 60 together with oleic acid and cholesterol using a thin-film hydration process based on full factorial design (24). The influence of formulation factors on UFAs’ physicochemical characteristics and the optimum formulation selection were investigated using Design-Expert® software. Based on the optimal UFA formulation, PRO–CTS–UFAs were constructed and characterized using transmission electron microscopy, stability studies, and ex vivo permeation. In vivo trials on rats with a sciatic nerve injury tested the efficacy of PRO–CTS–UFA and PRO–UFA transdermal hydrogels, PRO solution, compared to normal rats. Additionally, oxidative stress and specific apoptotic biomarkers were assessed, supported by a sciatic nerve histopathological study. PRO–UFAs and PRO–CTS–UFAs disclosed entrapment efficiency of 82.72 ± 2.33% and 85.32 ± 2.65%, a particle size of 317.22 ± 6.43 and 336.12 ± 4.9 nm, ζ potential of −62.06 ± 0.07 and 65.24 ± 0.10 mV, and accumulatively released 70.95 ± 8.14% and 64.03 ± 1.9% PRO within 6 h, respectively. Moreover, PRO–CTS–UFAs significantly restored sciatic nerve structure, inhibited the cisplatin-dependent increase in peripheral myelin 22 gene expression and MDA levels, and further re-established sciatic nerve GSH and CAT content. Furthermore, they elicited MBP re-expression, BCL-2 mild expression, and inhibited TNF-α expression. Briefly, our findings proposed that CTS–UFAs are promising to enhance PRO transdermal delivery to manage sciatic nerve damage.

show abstract

Section: Resultsmentioning

confidence: 99%

Sustainable Release of Propranolol Hydrochloride Laden with Biconjugated-Ufasomes Chitosan Hydrogel Attenuates Cisplatin-Induced Sciatic Nerve Damage in In Vitro/In Vivo Evaluation

et al. 2022

View full text Add to dashboard Cite

show abstract

“…By using a model stratum corneum membrane containing bovine brain ceramide, cholesterol and palmitic acid, Rowat and co-workers have also found that oleic acid can promote phase separation in the membrane, leading to changes in the structure and permeability of the stratum corneum [ 15 ]. Along with the fact that oleic acid can enhance skin permeation by stimulating epidermal lipid bilayer fluidization and corneocyte shrinkage via keratin condensation [ 16 ], leading to the enlargement of aqueous pores for transdermal drug delivery [ 16 ], it is expected that the oleic acid-containing vesicles can facilitate the transport of hydrophilic drugs across the skin. To examine the efficiency of the vesicles as skin permeation enhancers, THSG is adopted as a hydrophilic drug model ( Figure 3 A).…”

Section: Resultsmentioning

confidence: 99%

“…Compared to plain drug, the use of the vesicles as carriers enhances the transdermal flux of THSG by around 4-folds ( Figure 3C). aqueous pores for transdermal drug delivery [16], it is expected that the oleic acid-containing vesicles can facilitate the transport of hydrophilic drugs across the skin. To examine the efficiency of the vesicles as skin permeation enhancers, THSG is adopted as a hydrophilic drug model ( Figure 3A).…”

Section: Characterization Of Oleic Acid-containing Vesicles As Transdmentioning

confidence: 99%

Ionically Crosslinked Complex Gels Loaded with Oleic Acid-Containing Vesicles for Transdermal Drug Delivery

2020

View full text Add to dashboard Cite

Skin is an attractive site for drug administration partly because of its easy accessibility and favorable properties (e.g., less invasiveness and high patient compliance) over some other common routes of administration. Despite this, the efficiency in transdermal drug delivery has been largely limited by poor skin permeation. To address this problem, this study reports the generation of oleic acid-containing vesicles, which can enhance the drug delivery efficiency while showing good stability and limited skin disruption. Upon being loaded into a complex gel, along with the incorporation of the polymer blending technique, a delivery system exhibiting tunable transdermal flux of 2,3,5,4′-tetrahydroxystilbene 2-O-β-D-glucoside is reported. Taking the good biocompatibility and tunable delivery performance into account, our system warrants further development and optimization for future applications in the treatment of skin diseases.

show abstract

“…We used two chemical penetration enhancers: OA and azone. OA can extract endogenous lipids from the skin to disrupt highly compact intercellular lipid accumulation and produce large aqueous pores in the stratum corneum to promote transdermal drug diffusion [ 37 ]. Azone can infiltrate the lipid bilayer between epidermal cells, changing the well-organized tissue, increasing the lipid fluidity of the stratum corneum, and boosting the drug permeation coefficient [ 38 , 39 ].…”

Section: Discussionmentioning

confidence: 99%

Losartan Potassium and Verapamil Hydrochloride Compound Transdermal Drug Delivery System: Formulation and Characterization

Chen

Sun

Qin

et al. 2022

IJMS

View full text Add to dashboard Cite

In this study, we developed a sustained-release transdermal delivery system containing losartan potassium (LP) and verapamil hydrochloride (VPH). LP and VPH have low bioavailability and long half-life. Therefore, the development of an optimum administration mode is necessary to overcome these drawbacks and enhance the antihypertensive effect. A transdermal diffusion meter was used to determine the optimal formulation of LP-VPH transdermal drug delivery systems (TDDS). Based on in vitro results, a sustained-release patch was prepared. Physical characteristics, including quality, stickiness, and appearance, were evaluated in vitro, while pharmacokinetics and skin irritation were evaluated in vivo. The results showed that 8.3% polyvinyl alcohol, 74.7% polyvinylpyrrolidone K30, 12% oleic acid-azone, and 5% polyacrylic acid resin II provided an optimized TDDS product for effective administration of LP and VPH. Furthermore, in vitro and in vivo release tests showed that the system continuously released LP and VPH for 24 h. The pharmacokinetic results indicated that although the maximum concentration was lower, both the area under the curve from 0–time and the mean residence time of the prepared patch were significantly higher than those of the oral preparations. Furthermore, the prepared LP-VPH transdermal patch showed good stability and no skin irritation. The developed LP-VPH TDDS showed a sustained-release effect and good characteristics and pharmacokinetics; therefore, it is an ideal formulation.

show abstract

Transdermal insulin delivery with microwave and fatty acids as permeation enhancers

Cited by 22 publications

References 42 publications

Sustainable Release of Propranolol Hydrochloride Laden with Biconjugated-Ufasomes Chitosan Hydrogel Attenuates Cisplatin-Induced Sciatic Nerve Damage in In Vitro/In Vivo Evaluation

Sustainable Release of Propranolol Hydrochloride Laden with Biconjugated-Ufasomes Chitosan Hydrogel Attenuates Cisplatin-Induced Sciatic Nerve Damage in In Vitro/In Vivo Evaluation

Ionically Crosslinked Complex Gels Loaded with Oleic Acid-Containing Vesicles for Transdermal Drug Delivery

Losartan Potassium and Verapamil Hydrochloride Compound Transdermal Drug Delivery System: Formulation and Characterization

Contact Info

Product

Resources

About