Enhancement and mechanism of transdermal absorption of terpene-induced propranolol hydrochloride

Ying, Cui; Li, Lingzhi; Zhang, Li; Li, Jianyu; Gu, Jun; Gong, Hui; Guo, Pei; Wei, Tong

doi:10.1007/s12272-011-0909-2

Cited by 31 publications

(17 citation statements)

References 28 publications

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“…It is suggested that the interaction between the drug and terpenes via hydrogen bonding contributes to the enhancement of the partition coefficient. Following treatment with terpenes, the concentration of PH in the SC increased as a result of a molecular complex formation between the drug and the terpene [19].…”

Section: Mechanism Of Actionmentioning

confidence: 99%

Natural Terpenes as Penetration Enhancers for Transdermal Drug Delivery

et al. 2016

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Abstract:The greatest hindrance for transdermal drug delivery (TDD) is the barrier property of skin, especially the stratum corneum (SC). Various methodologies have been investigated and developed to enhance the penetration of drugs through the skin. Among them, the most popular approach is the application of penetration enhancers (PEs), including natural terpenes, a very safe and effective class of PEs. In the present paper, we focused on terpenes as skin PEs for TDD. The mechanism of their action, the factors affecting their penetration enhancement effect, as well as their possible skin toxicity were discussed. Terpenes abundant in nature have great potential in the development of PEs. Compared to synthetic PEs, natural terpenes have been proved to possess higher enhancement activity. Interaction with SC intercellular lipids is the main mechanism of action for terpenes. The key factor affecting the enhancement effect is the lipophilicity of both terpenes and drug molecules. In addition, a lot of terpenes have also been proved to be much less toxic compared to azone, the classic synthetic PE. In summary, terpenes may be preferred over the chemically synthesized compounds as safe and effective PEs to promote the percutaneous absorption of drugs.

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Section: Mechanism Of Actionmentioning

confidence: 99%

Natural Terpenes as Penetration Enhancers for Transdermal Drug Delivery

et al. 2016

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“…Since drugs could be directly delivered into CNS bypassing the blood-brain barrier via intranasal administration, this route was considered to be an attractive alternative to traditional injection therapy for CNS disorders. Previous studies have shown that borneol could enhance drug permeation through skin [11], gastrointestinal mucous membrane [12], nasal mucosa and cornea [13], [14].…”

Section: Introductionmentioning

confidence: 99%

Enhancing Effect of Borneol and Muscone on Geniposide Transport across the Human Nasal Epithelial Cell Monolayer

Chen

Gong

et al. 2014

PLoS ONE

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Geniposide is widely used in the treatment of cerebral ischemic stroke and cerebrovascular diseases for its anti-thrombotic and anti-inflammatory effects. Recent studies demonstrated that geniposide could be absorbed promptly and thoroughly by intranasal administration in mice and basically transported into the brain. Here, we explored its transport mechanism and the effect of borneol and muscone on its transport by human nasal epithelial cell (HNEC) monolayer. The cytotoxicity of geniposide, borneol, muscone and their combinations on HNECs was evaluated by the MTT assay. Transcellular transport of geniposide and the influence of borneol and muscone were studied using the HNEC monolayer. Immunostaining and transepithelial electrical resistance were measured to assess the integrity of the monolayer. The membrane fluidity of HNEC was evaluated by fluorescence recovery after photobleaching. Geniposide showed relatively poor absorption in the HNEC monolayer and it was not a P-gp substrate. Geniposide transport in both directions significantly increased when co-administrated with increasing concentrations of borneol and muscone. The enhancing effect of borneol and muscone on geniposide transport across the HNEC may be attributed to the significant enhancement on cell membrane fluidity, disassembly effect on tight junction integrity and the process was reversible. These results indicated that intranasal administration has good potential to treat cerebrovascular diseases.

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“…X-ray diffraction and differential scanning calorimetry (DSC) results showed that terpenes lead to increased drug penetration by disrupting the tight bilayers and lipid packing in the SC [46]. Furthermore, breaking the hydrogen bonds and extracting SC lipids [47], enhancing the partition into the SC by improving lipid fluidity [48] and increasing diffusion via the intercellular lipids [49] are another mechanisms that have been reported to increase drug permeability by terpenes.…”

Section: Effect Of Terpene On Penetrationmentioning

confidence: 99%

Invasome: A Novel Nanocarrier for Transdermal Drug Delivery

Babaie

Bakhshayesh

et al. 2020

Nanomaterials

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Invasomes are novel vesicular systems that exhibit improved transdermal penetration compared to conventional liposomes. These vesicles contain phospholipids, ethanol, and terpene in their structures; these components confer suitable transdermal penetration properties to the soft vesicles. The main advantages of these nanovesicles lie in their ability to increase the permeability of the drug into the skin and decrease absorption into the systemic circulation, thus, limiting the activity of various drugs within the skin layer. In this paper, several features of invasomes, including their structure, mechanism of penetration, applications, characterization, and potential advantages in dermal drug delivery, are highlighted. Overall, this review suggests that enhanced transdermal penetration of drugs using invasomes provides an appropriate opportunity for the development of lipid vesicular carriers.

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Enhancement and mechanism of transdermal absorption of terpene-induced propranolol hydrochloride

Cited by 31 publications

References 28 publications

Natural Terpenes as Penetration Enhancers for Transdermal Drug Delivery

Natural Terpenes as Penetration Enhancers for Transdermal Drug Delivery

Enhancing Effect of Borneol and Muscone on Geniposide Transport across the Human Nasal Epithelial Cell Monolayer

Invasome: A Novel Nanocarrier for Transdermal Drug Delivery

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