Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.1.1. Microstructure Patch Production Method
2.1.2. Skin Sample Preparation
2.1.3. Skin Treatment Using MSts
2.2. Characterisation of MSts and Skin Penetration
2.2.1. MSts Penetration Efficacy
2.2.2. Monitoring the Diffusion of Fluorescent DiI Using MSts
2.2.3. Monitoring the Diffusion of Fluorescein Hyaluronic Acid Using MSts
2.2.4. In Vitro Permeation Studies of APIs
2.2.5. Drug Solubility and Choice of Franz Cell Receptor Buffer
2.3. Detection and Quantification of Molecules
2.3.1. Detection and Quantification of BSA Using a Colorimetric Assay
2.3.2. Detection and Quantification of APIs Using HPLC
2.3.3. Calibration Curve
2.3.4. Data Analysis
3. Results
3.1. Characterisation of MSts and Skin Penetration
3.1.1. Characterisation of MSt Dimensions
3.1.2. MSt Penetration Efficacy
3.1.3. Characterisation of DiI Skin Permeation Using Polymer-Based Solid Microstructures (MSts).
3.1.4. Characterisation of F-HA Skin Permeation Using MSts
3.2. In Vitro Permeation Studies
4. Discussion
5. Conclusions
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Drug Name | Molecular Size (Da) | Partition Coefficient (LogP) | Acid Dissociation Constant (pKa) | Melting Point | Solubility in Water pH 7.4 (mg/mL) |
---|---|---|---|---|---|
Aspirin | 180 | 1.2 | 3.5 | 135 | 7.5 |
Galantamine | 368 | 1.8 | 8.2 | 126 | 20 |
Sel-HCl | 223 | 2.8 | 6.88 | 142 | 100 |
Insulin | 5808 | - | - | 80 | Insoluble |
Caffeine | 194 | −0.07 | 14 | 235 | 20 |
HC | 362 | 1.6 | 13.81 | 220 | Insoluble |
HC-HS | 484 | 1.6 | 5.64 | - | 100 |
BSA | 66,000 | - | - | 56 | 300 |
Drug | Solvent | Solubility (mg/mL) | Franz Cell Receptor Fluid | Initial Drug Quantity on Franz Cell (μg) |
---|---|---|---|---|
Aspirin | PBS | 7.5 | PBS | 3000 |
Galantamine | PBS | 20 | PBS | 6000 |
Sel-HCl | PBS | 100 | PBS | 20,000 |
Insulin | 0.01 M HCL | 12.5 | 0.01 M HCL | 5000 |
Caffeine | PBS | 20 | PBS | 2000 |
HC | Ethanol | 12.5 | PBS | 3750 |
HC-HS | PBS | 100 | PBS | 20,000 |
BSA | PBS | 300 | PBS | 120,000 |
Drug | Mobile Phase | Run Time (min) | Retention Time (min) | Wavelength (nm) |
---|---|---|---|---|
Aspirin | (A) methanol 30%, (B) 0.1% acetic acid 70% | 20 | 8.5 | 210 |
Galantamine | (A) acetonitrile 25%, (B) 0.1% TFA 75% | 10 | 2.4 | 220 |
Sel-HCl | (A) Methanol 35%, (B) 0.1% acetic acid 65% | 10 | 2.2 | 210 |
Insulin | (A) Acetonitrile 70%, (B) 0.1% TFA 30% | 15 | 2.2 | 210 |
Caffeine | (A) methanol 55%, (B) 0.1% acetic acid 45% | 5 | 2.4 | 274 |
HC | (A) methanol 70%, (B) 0.1% acetic acid 30% | 6 | 2.5 | 254 |
HC-HS | (A) Methanol 70%, (B) 0.1% acetic acid 30% | 10 | 4.5 | 254 |
Drug Name | Cumulative Amount at 24 h (μg) | Flux (μg/cm2/h) | Permeation at 24 h (%) | ER | |||
---|---|---|---|---|---|---|---|
+ MSt | Control | + MSt | Control | + MSt | Control | ||
Aspirin | 452 ± 210 | 134 ± 38 | 77 ± 35 | 3.4 ± 0.5 | 15 ± 7 | 3 ± 1 | 4.8 ± 0.8 |
Galantamine | 1188 ± 290 | 67 ± 23 | 49 ± 8 | 0.7 ± 0.6 | 20 ± 5 | 1 ± 0.4 | 21 ± 3.6 |
Sel-HCl | 1974 ± 511 | 373 ± 77 | 43 ± 12 | 11 ± 2 | 10 ± 2.5 | 1.9 ± 0.4 | 5.2 ± 0.2 |
Insulin | 1515 ± 120 | 1188 ± 137 | 85 ± 8 | 89 ± 6 | 30 ± 2.4 | 23 ± 2.8 | 1.3 ± 0.03 |
Caffeine | 1383 ± 176 | 356 ± 149 | 308 ± 18 | 26 ± 5 | 70 ± 8 | 18 ± 7 | 4.2 ± 1.3 |
HC | 73 ± 47 | 6 ± 3 | 11 ± 4 | 3 ± 0.7 | 2.3 ± 1.3 | 0.1 ± 0.08 | 22.3 ± 10.8 |
HC-HS | 1691 ± 818 | 53 ± 13 | 64 ± 21 | 2 ± 0.03 | 8.4 ± 4 | 0.2 ± 0.06 | 40.4 ± 8.2 |
BSA | 16275 ± 3078 | 2792 ± 576 | 8133 ± 1365 | 188 ± 19 | 14 ± 2.5 | 2 ± 0.5 | 7.1 ± 0.5 |
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Rahbari, R.; Ichim, I.; Bamsey, R.; Burridge, J.; Guy, O.J.; Bolodeoku, J.; Graz, M. Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs. Pharmaceutics 2020, 12, 1213. https://doi.org/10.3390/pharmaceutics12121213
Rahbari R, Ichim I, Bamsey R, Burridge J, Guy OJ, Bolodeoku J, Graz M. Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs. Pharmaceutics. 2020; 12(12):1213. https://doi.org/10.3390/pharmaceutics12121213
Chicago/Turabian StyleRahbari, Raha, Ionut Ichim, Ryan Bamsey, Jemma Burridge, Owen J. Guy, John Bolodeoku, and Michael Graz. 2020. "Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs" Pharmaceutics 12, no. 12: 1213. https://doi.org/10.3390/pharmaceutics12121213