Transdermal Delivery of Lercanidipine Hydrochloride: Effect of Chemical Enhancers and Ultrasound

Shetty, Pallavi K.; Suthar, Neelam A.; Menon, Jyothsna; Deshpande, Praful Balavant; Avadhani, Kiran; Kulkarni, Raghavendra V.; Mutalik, Srinivas

doi:10.2174/1567201811310040007

Cited by 16 publications

(4 citation statements)

References 27 publications

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“…Furthermore, spreadability of nanoemulgel has been examined as it is considered an important test to investigate the maximum slip and drag of transdermal formulations, that would reflect its ease of application. 52 The spreadability was found to be 6.73 ± 0.12 g.cm.s -1 , thereby, indicating an easily spreadable formulation. 34 …”

Section: Resultsmentioning

confidence: 86%

Transdermal Delivery of Capsaicin Nanoemulgel: Optimization, Skin Permeation and in Vivo Activity Against Diabetic Neuropathy

2021

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Purpose: Diabetic somatic neuropathy is one of the most prevalent complications in type 1 diabetes mellitus. Many treatments were investigated to alleviate the pain associated with this condition. Capsaicin is a naturally occurring lipophilic alkaloid that proved to be an effective and safe treatment of chronic painful disorders. Despite the known therapeutic benefits of capsaicin, the conventional topical formulations have limited bioavailability. Therefore, the current study aims to develop capsaicin nanoemulgel to increase skin permeation and enhance its activity against neuropathic pain. Methods: Low-energy emulsification method was used to prepare nanoemulsions, using eucalyptus oil as the oily phase, tween 80 as a surfactant, propylene glycol, ethanol and isopropyl alcohol as co-surfactants. Pseudo-ternary phase diagrams were constructed to investigate and optimize the formulation. Subsequently, the optimum formulation was formulated as a nanoemulgel and investigated for, skin permeation using Franz diffusion cell, and diabetic neuropathy management using alloxan-induced diabetic mice. Results: The selected nanoemulsion containing 0.05% capsaicin is composed of 8 % oil, 24 % Smix (Tween 80: isopropyl alcohol 2:1 w/w) and 68 % water. It is characterized by nanosized globules (28.15±0.24 nm) with a relatively low polydispersity index (0.27±0.05). The nanoemulgel revealed circa 4-fold increase in capsaicin cumulative permeation when compared to the conventional gel, and an improvement in its antinociceptive properties was observed in the treated diabetic mice (p<0.05). Conclusion: The selected capsaicin nanoemulgel would be a promising transdermal formulation that may alleviate diabetic neuropathy in type 1 diabetes mellitus patients.

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Section: Resultsmentioning

confidence: 86%

Transdermal Delivery of Capsaicin Nanoemulgel: Optimization, Skin Permeation and in Vivo Activity Against Diabetic Neuropathy

2021

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“…As stated earlier, the existing work in the literature suggests that it is possible to combine 130 more than one method for enhancing drug permeability and there is a significant amount of 131 work on different combinational approaches [40,41]. However, it needs to be pointed out 132 that the researches on the development of individual technology are very important for the 133 development of the combinational methods because the researches on the individual method 134 Fig.…”

Section: Different Tdd Technologiesmentioning

confidence: 99%

Potential of combined ultrasound and microneedles for enhanced transdermal drug permeation: A review

Han

Das

2015

European Journal of Pharmaceutics and Biopharmaceutics

135

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Citation: HAN, T. and DAS, D.B., 2015. Potential of combined ultrasound and microneedles for enhanced transdermal drug permeation: a review. European Journal of Pharmaceutics and Biopharmaceutics,89, Additional Information:• NOTICE: this is the author's version of a work that was accepted for publication in European Journal of Pharmaceutics and Biopharmaceutics. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive ver- have been developed to overcome the resistance of the stratum corneum to molecular 10 diffusion. In particular, researchers have started to consider the possibility of combining the 11 TDD technologies in order to have further increase in drug permeability. Microneedles (MNs) 12 and ultrasound are both promising technologies. They achieve enhancement in drug 13 permeation via different mechanisms and therefore give a good potential for combining with 14 each other. This review will focus on discussing the potential of this combinational technique 15 along with other important issues, e.g., the mechanisms of ultrasound and MNs as it is these 16 mechanisms which are coupled via the two systems (i.e. MNs and ultrasound). We discuss 17 the possible ways to achieve this combination as well as how this combination would 18 increase the permeability. Some of the undeveloped (weaker) research areas of MNs and 19 sonophoresis are also discussed in order to understand the true potential of combining the two 20 technologies when they are developed further in the future. We propose several hypothetical 21 combinations based on the possible mechanisms involved in MNs and ultrasound. 22Furthermore, we carry out a cluster analysis by which we determine the significance of this 23Page 2 of 54 combinational method in comparison with some other selected combinational methods for 24 TDD (e.g., MNs and iontophoresis). Using a time series analysis tool (ARIMA model), the 25 current trend and the future development of combined MNs and ultrasound are also analysed. 26Overall, the review in this paper indicates that combining MNs and ultrasound is a promising 27 TDD method for the future. 28

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“…The partition coefficient values of drugs in n-octanol/water were determined 20,21 . Then, 20 mL of n-octanol (saturated with water) was added to an equivalent volume of coarse drugs saturated solution in water (saturated with n-octanol) in a separating funnel.…”

Section: Determination Of Log Pmentioning

confidence: 99%

Influence of drug physicochemical characteristics onin vitrotransdermal absorption of hydrophobic drug nanosuspensions

Shen¹,

Li²,

Shen³

et al. 2015

Drug Development and Industrial Pharmacy

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The purpose of this paper was to study the influence of drug physicochemical characteristics on in vitro transdermal absorption of hydrophobic drug nanosuspensions. Four drug nanosuspensions were produced by high-pressure homogenization technique, which were the same in stabilizer and similar in particle size. Differential scanning calorimetry and powder X-ray diffraction analysis showed that the crystalline state of the nanocrystals did not change. In vitro permeation study demonstrated that the drug nanosuspensions have a higher rate of permeation that ranged from 1.69- to 3.74-fold compared to drug microsuspensions. Correlation analysis between drug physicochemical properties and Jss revealed that log P and pKa were factors that influenced the in vitro transdermal absorption of hydrophobic drug nanosuspensions, and drugs with a log P value around 3 and a higher pKa value (when pKa < pH+2) would gain higher Jss in this paper.

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Transdermal Delivery of Lercanidipine Hydrochloride: Effect of Chemical Enhancers and Ultrasound

Cited by 16 publications

References 27 publications

Transdermal Delivery of Capsaicin Nanoemulgel: Optimization, Skin Permeation and in Vivo Activity Against Diabetic Neuropathy

Transdermal Delivery of Capsaicin Nanoemulgel: Optimization, Skin Permeation and in Vivo Activity Against Diabetic Neuropathy

Potential of combined ultrasound and microneedles for enhanced transdermal drug permeation: A review

Influence of drug physicochemical characteristics onin vitrotransdermal absorption of hydrophobic drug nanosuspensions

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