Transdermal delivery of rapamycin with poor water-solubility by dissolving polymeric microneedles for anti-angiogenesis

Mao, Jinzhu; Wang, Hua; Xie, Ying; Fu, Yangxue; Li, Yuce; Liu, Pei; Du, Hui; Zhu, Jinjin; Dong, Liyun; Hussain, Mubashir; Li, Yan; Zhang, Lianbin; Zhu, Jintao; Tao, Juan

doi:10.1039/c9tb00912d

Cited by 41 publications

(20 citation statements)

References 31 publications

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“…Animal Models. Most pharmacological studies are conducted through in vivo animal models [ 46 , 50 , 220 , 221 , 222 , 223 ]. The animal fur was removed from the anesthetized animal, and the MN patch was subsequently applied to the underlying skin.…”

Section: Pharmacokinetic and Drug Release Behavior From Polymeric Mnsmentioning

confidence: 99%

Translation of Polymeric Microneedles for Treatment of Human Diseases: Recent Trends, Progress, and Challenges

Yadav

Munni²,

Campbell

et al. 2021

Pharmaceutics

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The ongoing search for biodegradable and biocompatible microneedles (MNs) that are strong enough to penetrate skin barriers, easy to prepare, and can be translated for clinical use continues. As such, this review paper is focused upon discussing the key points (e.g., choice polymeric MNs) for the translation of MNs from laboratory to clinical practice. The review reveals that polymers are most appropriately used for dissolvable and swellable MNs due to their wide range of tunable properties and that natural polymers are an ideal material choice as they structurally mimic native cellular environments. It has also been concluded that natural and synthetic polymer combinations are useful as polymers usually lack mechanical strength, stability, or other desired properties for the fabrication and insertion of MNs. This review evaluates fabrication methods and materials choice, disease and health conditions, clinical challenges, and the future of MNs in public healthcare services, focusing on literature from the last decade.

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Section: Pharmacokinetic and Drug Release Behavior From Polymeric Mnsmentioning

confidence: 99%

Translation of Polymeric Microneedles for Treatment of Human Diseases: Recent Trends, Progress, and Challenges

Yadav

Munni²,

Campbell

et al. 2021

Pharmaceutics

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“…Over the last years, many efforts have been devoted to the design of high-performance drug delivery systems capable to transport suitable dosage of the drug with high spatial and temporal accuracy. As is well-known, drugs administered through conventional routes may lead to a series of unwanted effects mainly induced by their poor water solubility in lipophilic solvents and insufficient bioavailability [ 1 , 2 , 3 , 4 , 5 , 6 , 7 ], strongly limiting their pharmacological efficacy. In this context, supramolecular compounds based on natural and modified cyclodextrins (CDs and MCDs, respectively) represent an attractive strategy for the engineering of bio-friendly host-guest inclusion complexes capable to improve the chemical/physical properties of pharmaceutical agents both in solution or in solid state [ 8 , 9 , 10 , 11 , 12 ].…”

Section: Introductionmentioning

confidence: 99%

Temperature-Dependent Dynamical Evolution in Coum/SBE-β-CD Inclusion Complexes Revealed by Two-Dimensional FTIR Correlation Spectroscopy (2D-COS)

et al. 2021

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A combination of Fourier transform infrared spectroscopy in attenuated total reflectance geometry (FTIR-ATR) and 2D correlation analysis (2D-COS) was applied here for the first time in order to investigate the temperature-dependent dynamical evolution occurring in a particular type of inclusion complex, based on sulfobutylether-β-cyclodextrin (SBE-β-CD) as hosting agent and Coumestrol (7,12-dihydorxcoumestane, Coum), a poorly-soluble active compound known for its anti-viral and anti-oxidant activity. For this purpose, synchronous and asynchronous 2D spectra were calculated in three different wavenumber regions (960–1320 cm−1, 1580–1760 cm−1 and 2780–3750 cm−1) and over a temperature range between 250 K and 340 K. The resolution enhancement provided by the 2D-COS offers the possibility to extract the sequential order of events tracked by specific functional groups of the system, and allows, at the same time, the overcoming of some of the limits associated with conventional 1D FTIR-ATR analysis. Acquired information could be used, in principle, for the definition of an optimized procedure capable to provide high-performance T-sensitive drug carrier systems for different applications.

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“…Since the first demonstration of the applicability of MN in 1998 [1], it has been recognised as an alternative to traditional methods for the delivery of vaccines, drugs and cosmetics [4]. For example, MNs have been employed recently to improve the transdermal permeation of insulin [5], caffeine [6], human growth hormone [7], lidocaine [8], ovalbumin [9], bovine albumin [10], bevacizumab [11], rapamycin [12], Calcein [13], parathyroid hormone [14] and levonorgestrel [15]. MNs have also been explored for the delivery of other molecules such as peptides, ocular drugs and cancer drugs [16].…”

Section: Introductionmentioning

confidence: 99%

“…While under (ii), various technologies such as micro-electromechanical systems (MEMS) [20,21], laser cutting [22,23], 3D printing [24,25], and lithography [26][27][28] have been applied for production of MN. transdermal permeation of insulin [5], caffeine [6], human growth hormone [7], lidocaine [8], ovalbumin [9], bovine albumin [10], bevacizumab [11], rapamycin [12], Calcein [13], parathyroid hormone [14] and levonorgestrel [15]. MNs have also been explored for the delivery of other molecules such as peptides, ocular drugs and cancer drugs [16].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Mathematical Modelling, Simulation and Optimisation of Microneedles for Transdermal Drug Delivery: Trends and Progress

et al. 2020

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In the last two decades, microneedles (MNs) have received significant interest due to their potential for painless transdermal drug delivery (TDD) and minimal skin damage. MNs have found applications in a range of research and development areas in drug delivery. They have been prepared using a variety of materials and fabrication techniques resulting in MN arrays with different dimensions, shapes, and geometries for delivery of a variety of drug molecules. These parameters play crucial roles in determining the drug release profiles from the MNs. Developing mathematical modelling, simulation, and optimisation techniques is vital to achieving the desired MN performances. These will then be helpful for pharmaceutical and biotechnological industries as well as professionals working in the field of regulatory affairs focusing on MN based TDD systems. This is because modelling has a great potential to reduce the financial and time cost of both the MNs’ studies and manufacturing. For example, a number of robust mathematical models for predicting the performance of the MNs in vivo have emerged recently which incorporate the roles of the structural and mechanical properties of the skin. In addressing these points, this review paper aims to highlight the current status of the MN modelling research, in particular, the modelling, simulation and optimisation of the systems for drug delivery. The theoretical basis for the simulation of MN enhanced diffusion is discussed within this paper. Thus, this review paper provides a better understanding of the modelling of the MN mediated drug delivery process.

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Transdermal delivery of rapamycin with poor water-solubility by dissolving polymeric microneedles for anti-angiogenesis

Abstract: Rapamycin-loaded dissolving microneedles (RAPA DMNs) are fabricated by using polyvinylpyrrolidone (PVP) as the matrix and exhibit the good anti-angiogenic effect.

Cited by 41 publications

References 31 publications

Translation of Polymeric Microneedles for Treatment of Human Diseases: Recent Trends, Progress, and Challenges

Translation of Polymeric Microneedles for Treatment of Human Diseases: Recent Trends, Progress, and Challenges

Temperature-Dependent Dynamical Evolution in Coum/SBE-β-CD Inclusion Complexes Revealed by Two-Dimensional FTIR Correlation Spectroscopy (2D-COS)

Mathematical Modelling, Simulation and Optimisation of Microneedles for Transdermal Drug Delivery: Trends and Progress

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