Curcumin In Situ Gelling Polymeric Insert with Enhanced Ocular Performance
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Preparation of Curcumin Ocular Inserts
2.2.1. Preparation of Polymer Solutions
2.2.2. Preparation of Curcumin Inserts
2.3. Characterization of Curcumin Inserts
2.3.1. Physicochemical, Mechanical, Morphological, Thermal, Spectroscopic and Mucoadhesive Characteristics
- Determination of mechanical properties [tensile strength, strain (%) and folding endurance]
- Surface morphology and topography studies of the prepared curcumin inserts
- Fourier transform infrared (FTIR) study
- Mucoadhesion Studies Using Excised Bovine Conjunctival Membrane
2.3.2. In Vitro Release Studies
2.3.3. Ex Vivo Permeation Using Porcine Corneal Models
2.3.4. Bovine Cornea Opacity and Permeability (BCOP) Test
2.3.5. Antioxidant Tests
- Trolox equivalent antioxidant capacity (TEAC) assay
- Cupric reducing antioxidant capacity (CUPRAC) test
2.3.6. In Vivo Ocular Residence Time of the Prepared Insert
2.4. Statistical Analysis
3. Results and Discussion
3.1. Preparation of Curcumin Inserts
3.2. Characterization of Curcumin Inserts
3.2.1. Weight, Thickness, Drug Content, Moisture Uptake, pH Measurements and Mechanical Characteristics of the Prepared Curcumin Inserts
3.2.2. Surface Morphology and Topography Studies
3.2.3. Thermal Behaviour (DSC Studies)
3.2.4. FT-IR Spectroscopy
3.2.5. Mucoadhesion Studies
3.2.6. In Vitro Release and Transcorneal Permeation of Curcumin
3.2.7. BCOP Assay
3.2.8. Antioxidant Assays
3.3. In Vivo Ocular Residence Time
4. Conclusions
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Formulation Code | F1 | F2 | F3 | F4 | F5 | F6 | F7 | F8 | F9 |
---|---|---|---|---|---|---|---|---|---|
Composition | |||||||||
Curcumin * (mg) | 20 | 20 | 20 | 15 | 15 | 15 | 20 | 20 | 20 |
PVA 5% w/w | 20 g | 20 g | 20 g | 10g | 10 g | 10 g | 10 g | 10 g | 10 g |
HPMC 2.5% w/w | 40 g | 40 g | 20 g | 20 g | 20 g | ||||
CMC 2.5% w/w | 40 g | 40 g | 20 g | 20 g | 20 g | ||||
PL 127 10% w/w | 10 g | 10 g | 5 g | 5 g | 5 g | ||||
GLY | 600 mg | 600 mg | 600 mg | 450 mg | 450 mg | 450 mg | 600 mg | ||
TEC | 600 mg | ||||||||
PEG 400 | 600 mg |
Formulation | F1 | F2 | F3 | F4 | F5 | F6 * | F7 | F8 | F9 |
---|---|---|---|---|---|---|---|---|---|
Thickness (µm) | 230 ± 12 | 270 ± 12 | 280 ± 16 | 230 ± 12 | 260 ± 10 | 270 ± 13 | 280 ± 18 | 290 ± 12 | |
Weight (mg) | 8 ± 0.2 | 13.5 ± 0.3 | 15 ± 0.3 | 8 ± 0.5 | 11 ± 0.4 | 14 ± 0.7 | 17 ± 0.8 | 15 ± 0.45 | |
Curcumin content (% w/w) | 0.95 ± 1.0 | 0.90 ± 0.2 | 0.75 ± 6 | 0.90 ± 0.1 | 0.90 ± 0.3 | 0.94 ± 0.1 | 0.85 ± 0.8 | 0.95 ± 0.2 | |
Surface pH | 7 | 7.5 | 7.5 | 7 | 7 | 7 | 7.5 | 7.5 | |
Moisture uptake (%) | 15 ± 0.2 | 22 ± 0.7 | 20 ± 1.2 | 32 ± 1.5 | 30 ± 2.0 | 25.0 ± 14 | 10 ± 1.4 | 15 ± 1.3 | |
Tensile strength (MPa) | 13 ± 1.5 | 15 ± 0.7 | 10 ± 2.6 | 5.6 ± 1.0 | 17 ± 1.5 | 5.2 ± 1.0 | 17 ± 0.7 | 18.8 ± 0.9 | |
Strain (%) | 61 ± 2.0 | 29.3 ± 2.5 | 58 ± 8.0 | 80 ± 10 | 13.6 ± 3.6 | 82 ± 2.4 | 22.5 ± 1.5 | 29 ± 3.0 | |
Folding endurance | 255 ± 8.4 | 391 ± 6.0 | 181 ± 10 | 205 ± 4.0 | 360 ± 8.0 | 380 ± 12 | 300 ± 7.0 | 315 ± 5.0 |
Formulation Code | In vitro Release Kinetics | Ex vivo Permeation | |||
---|---|---|---|---|---|
* RRT300 min | n | R2 | Flux (µg.cm−2.h−1) | Papp × 10−6 (cm/s) | |
Curcumin suspension | - | - | - | 0.27 ± 0.01 | 0.07 ± 0.008 |
F5 | 8.7 | 0.52 | 0.994 | 1.86 ± 0.05 | 0.51 ± 0.01 |
F7 | 9 | 0.44 | 0.98 | 2.20 ± 0.1 | 0.60 ± 0.01 |
F8 | 9 | 0.51 | 0.99 | 2.24 ± 0.15 | 0.62 ± 0.02 |
F9 | 7.5 | 0.44 | 0.99 | 1.36 ± 0.09 | 0.42 ± 0.006 |
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Abdelkader, H.; Wertheim, D.; Pierscionek, B.; Alany, R.G. Curcumin In Situ Gelling Polymeric Insert with Enhanced Ocular Performance. Pharmaceutics 2020, 12, 1158. https://doi.org/10.3390/pharmaceutics12121158
Abdelkader H, Wertheim D, Pierscionek B, Alany RG. Curcumin In Situ Gelling Polymeric Insert with Enhanced Ocular Performance. Pharmaceutics. 2020; 12(12):1158. https://doi.org/10.3390/pharmaceutics12121158
Chicago/Turabian StyleAbdelkader, Hamdy, David Wertheim, Barbara Pierscionek, and Raid G. Alany. 2020. "Curcumin In Situ Gelling Polymeric Insert with Enhanced Ocular Performance" Pharmaceutics 12, no. 12: 1158. https://doi.org/10.3390/pharmaceutics12121158