Electroporation-enhanced transdermal drug delivery: Effects of logP, pKa, solubility and penetration time

Chen, Xiao; Zhu, Lin; Li, Ruiteng; Pang, Lulu; Zhu, Siqing; Ma, Jinqiu; Du, Lina; Jin, Yiguang

doi:10.1016/j.ejps.2020.105410

Cited by 49 publications

(19 citation statements)

References 50 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This method uses the application of high voltage electric pulses ranging from 5 to 500 V for short exposure times (~ms) to the skin, which leads to the formation of small pores in the SC that improve permeability and aid drug diffusion [ 34 , 35 ]. For safe and painless drug administration, electric pulses are introduced using closely positioned electrodes.…”

Section: Enhancement Of Transdermal Delivery By Equipment (Active Delivery)mentioning

confidence: 99%

Recent advances in transdermal drug delivery systems: a review

et al. 2021

View full text Add to dashboard Cite

Various non-invasive administrations have recently emerged as an alternative to conventional needle injections. A transdermal drug delivery system (TDDS) represents the most attractive method among these because of its low rejection rate, excellent ease of administration, and superb convenience and persistence among patients. TDDS could be applicable in not only pharmaceuticals but also in the skin care industry, including cosmetics. Because this method mainly involves local administration, it can prevent local buildup in drug concentration and nonspecific delivery to tissues not targeted by the drug. However, the physicochemical properties of the skin translate to multiple obstacles and restrictions in transdermal delivery, with numerous investigations conducted to overcome these bottlenecks. In this review, we describe the different types of available TDDS methods, along with a critical discussion of the specific advantages and disadvantages, characterization methods, and potential of each method. Progress in research on these alternative methods has established the high efficiency inherent to TDDS, which is expected to find applications in a wide range of fields.

show abstract

Section: Enhancement Of Transdermal Delivery By Equipment (Active Delivery)mentioning

confidence: 99%

Recent advances in transdermal drug delivery systems: a review

et al. 2021

View full text Add to dashboard Cite

show abstract

“…Typically, for a successful salt formation, the required difference between the p K a values of an acid and a base should be >2 . The p K a value of metformin is 10.59, and the reported p K a values for caprate, laurate, oleate, cholate, and docusate are 4.9, 4.95, 5, 4.98, and −0.75, respectively . Thus, the difference in the p K a values of metformin and the counterions was large enough to allow for the salt formation.…”

Section: Discussionmentioning

confidence: 99%

Synthesis and Characterization of Lipophilic Salts of Metformin to Improve Its Repurposing for Cancer Therapy

et al. 2021

View full text Add to dashboard Cite

Epidemiological evidence has accentuated the repurposing of metformin hydrochloride for cancer treatment. However, the extreme hydrophilicity and poor permeability of metformin hydrochloride are responsible for its poor anticancer activity in vitro and in vivo. Here, we report the synthesis and characterization of several lipophilic metformin salts containing bulky anionic permeation enhancers such as caprate, laurate, oleate, cholate, and docusate as counterions. Of various counterions tested, only docusate was able to significantly improve the lipophilicity and lipid solubility of metformin. To evaluate the impact of the association of anionic permeation enhancers with metformin, we checked the in vitro anticancer activity of various lipophilic salts of metformin using drug-sensitive (MYCN-2) and drug-resistant (SK-N-Be2c) neuroblastoma cells as model cancer cells. Metformin hydrochloride showed a very low potency (IC 50 ≈ >100 mM) against MYCN-2 and SK-N-Be2c cells. Anionic permeation enhancers showed a considerably higher activity (IC 50 ≈ 125 μM to 1.6 mM) against MYCN-2 and SK-N-Be2c cells than metformin. The association of metformin with most of the bulky anionic agents negatively impacted the anticancer activity against MYCN-2 and SK-N-Be2c cells. However, metformin docusate showed 700-to 4300-fold improvement in anticancer potency compared to metformin hydrochloride and four-to five-fold higher in vitro anticancer activity compared to sodium docusate, indicating a synergistic association between metformin and docusate. A similar trend was observed when we tested the in vitro activity of metformin docusate, sodium docusate, and metformin hydrochloride against hepatocellular carcinoma (HepG2) and triple-negative breast cancer (MDA-MB-231) cells.

show abstract

“…Another technique is magnetophoresis, in which electric charges induce a magnetic field and with this occurs the vectorization of the drug [71]. We also have electroporation; in this technique, an aqueous pore is created in the skin by exposing it to high voltages for short periods, allowing the entry of bioactive compounds [72]. Finally, we find microporation, which, like electroporation, is based on creating a pore that will enable the passage of bioactive compounds.…”

Section: Transdermal Administration Based On Electrical Techniquesmentioning

confidence: 99%

The Importance of Nanocarrier Design and Composition for an Efficient Nanoparticle-Mediated Transdermal Vaccination

et al. 2021

View full text Add to dashboard Cite

The World Health Organization estimates that the pandemic caused by the SARS-CoV-2 virus claimed more than 3 million lives in 2020 alone. This situation has highlighted the importance of vaccination programs and the urgency of working on new technologies that allow an efficient, safe, and effective immunization. From this perspective, nanomedicine has provided novel tools for the design of the new generation of vaccines. Among the challenges of the new vaccine generations is the search for alternative routes of antigen delivery due to costs, risks, need for trained personnel, and low acceptance in the population associated with the parenteral route. Along these lines, transdermal immunization has been raised as a promising alternative for antigen delivery and vaccination based on a large absorption surface and an abundance of immune system cells. These features contribute to a high barrier capacity and high immunological efficiency for transdermal immunization. However, the stratum corneum barrier constitutes a significant challenge for generating new pharmaceutical forms for transdermal antigen delivery. This review addresses the biological bases for transdermal immunomodulation and the technological advances in the field of nanomedicine, from the passage of antigens facilitated by devices to cross the stratum corneum, to the design of nanosystems, with an emphasis on the importance of design and composition towards the new generation of needle-free nanometric transdermal systems.

show abstract

Electroporation-enhanced transdermal drug delivery: Effects of logP, pKa, solubility and penetration time

Cited by 49 publications

References 50 publications

Recent advances in transdermal drug delivery systems: a review

Recent advances in transdermal drug delivery systems: a review

Synthesis and Characterization of Lipophilic Salts of Metformin to Improve Its Repurposing for Cancer Therapy

The Importance of Nanocarrier Design and Composition for an Efficient Nanoparticle-Mediated Transdermal Vaccination

Contact Info

Product

Resources

About