Table 1. Overview of thermally evaporated different drug substances.
Test Material; Indication and potential use of solvent free nanostructuring by TE | Melting point at atmosphere (typical evaporation temperature range) [°C]} | Deposition remarks | Maximum extent of inhibition area (cm2) [TE deposited on titan plates] | Maximum extent of inhibition area (cm2)[Control (paper, 30 µg/disc)] |
1. Chloramphenicol; Antibiotic, Increased solubility | 150 (∼90–118) | Crystalline deposits | 2.55 (S.* aureus); Amount<30 µg | 1.36 |
2. Erythromycin (base); Antibiotic, Increased oral bioavailability | 190–193 (∼100–137) | Amorphous and crystalline deposits; Raman spectra | 3.11 (S. aureus); Amount<30 µg | 1.38 |
3. Metronidazole; Antibiotic, Dental implant coating | 159–163 (∼100–194) | Crystalline deposits; Raman spectra | 2.06 (S. aureus); Prove of prin-ciple, amount not further quantified | 1.67 |
4. Propyl-p-hydroxybenzoate (Nipasol); Preservative, pre-preserved container | 95–98 (∼85–165) | Crystalline deposits | 1.16 (S. aureus); Prove of prin-ciple, amount not further quantified | Under progress |
5. Neomycin sulphate; Antibiotic, Surface coating of wound dressings/implants | 250–260 (∼160–300) | Amorphous and crystalline deposits | 0.57 (S. aureus) Amount<30 µg | 0.68 |
6. Novobiocin sodium salt; Antibiotic, Surface coating of wound dressings/implants | 215–220 (∼150–250) | Amorphous and crystalline deposits | 3.95 (S. aureus) Amount<30 µg | 1.64 |
7. Tetracycline hydrate; Antibiotic, Device coating | 170–175 (∼100–223) | Crystalline deposits | 1.44 (S. aureus) Amount∼3.25 µg | 1.82 |
8. Tetracycline HCl; Antibiotic, Device coating | 220–223 (∼119–255) | Crystalline deposits | 1.65 (S. aureus) Amount<30 µg | Under progress |
9. Vancomycin HCl; Antibiotic, Increased oral bioavailability | 185 (∼100–197) | Amorphous and crystalline deposits | 0.67 (S. aureus) Amount<30 µg | 0.80 |
10. Clotrimazole; Antimycotic, Improved nail coating | 147–149 (∼89–164) | Crystalline deposits; Raman spectra | 1.76 (Candida albicans); Proveof principle, amount notfurther quantified | 1.72 |
11. Itraconazole; Antimycotic, Increased oral bioavailability | 166,2 (∼100–232) | Amorphous and crystalline deposits | 1.82 (Candida albicans) Proveof principle, amount notfurther quantified | 0.97 |
12. Ketoconazole; Antimycotic, increased solubility | 146 (∼88–226) | Amorphous and crystalline deposits | 2.83 (Candida albicans)Amount <30 µg | 1.07 |
13. Pindolol; Beta blocker, Contact lens coating | 167–171 (∼110–215) | Crystalline deposits/Raman Spectra | ||
14. Pilocarpine HCl; Parasympatho-mimetic, Contact lens coating | 200–203 (∼117–250) | Crystalline deposits/Raman Spectra | ||
15. Cholesterol; Excipient, Biocompatible protection layer | 148–150 (∼90–165) | Crystalline deposits | ||
16. PLGA Excipient, Controlled release layer | 224–226 (∼ 150–300) | Amorphous deposits | ||
17. 5-Fluorouracil; Antimetabolite (Anticancer) | 283 (∼115–250) | Crystalline deposits | ||
18. Sulfathiazole; Oral and topical antibiotic | 200–203 (∼110–250) | Crystalline deposits | ||
19. Acetyl salicylic acid (ASS); Non steroidal anti-inflammatory drug | 135 (∼90–140) | Crystalline deposits | ||
20. Paracetamol; Non steroidal anti-inflammatory drug | 168 (∼97–130) | Crystalline deposits | ||
21. Diclofenac sodium; Non steroidal anti-inflammatory drug | 284 (∼135–270) | Crystalline deposits/Raman spectra | ||
22. Ascorbic acid Antioxidant | 190–192 (∼123–200) | Crystalline deposits | ||
22. Tetracaine HCl; Local anaesthetic | 149 (∼114–220) | Crystalline deposits | ||
23. Trimethoprim; Antibiotic | 199–203 (∼100–170) | Amorphous and crystalline deposits | ||
24. Indometacin; Non steroidal anti-inflammatory drug | 155 (∼150–190) | Amorphous and crystalline deposits | ||
25. Polyglycolic acid; Biodegradable polymer, Control drug release | 225–230 (∼160–200) | Amorphous and crystalline deposits | ||
26. Adipic acid; Excipient | 152.1(∼119) | Crystalline deposits | ||
27. Caffeine; Psychoactive stimulant drug, Excipient | 227–228 (∼120–250) | Crystalline deposits | ||
28. Lactose Excipient | 223 | Deposition not possible | ||
29. Polyethylene glycol; Excipient | 49–53 | Deposition not possible (decomposed to gas) | ||
30. Chlorhexidine; Antiseptic | 134–136 | Decomposes, droplets on the surface of substrate | ||
31. Triclosan; Antibacterial and antifungal agent | 56–58 | Deposition not possible (Degrades to dioxin) |
First part (1–12) lists the materials which has been successfully nanostructured by thermal evaporation and have been tested with disk diffusion method. The second part (13–27) lists the successfully deposited materials however the biological tests are under progress. The last part (28–31) lists the pharmaceutical substances which are not suitable for thermal evaporation as they are decomposed during deposition. (*Staphylococcus).