Table 2.
Examples of some inhaled sustained drug release formulations used to treat both local lung diseases and systemic diseases.
| Disease | API | Main excipient used | Type of sustained release formulations | Therapeutic outcome | Stage | Ref. |
|---|---|---|---|---|---|---|
| Local lung diseases | ||||||
| Asthma | Budesonide | PLGA, poly(vinylpyrrolidone) | Large porous particles | The formulation significantly reduced the total number of inflammatory cells and expression of IL-4 and IL-5 in BALF as compared to the physical mixture (budesonide/lactose). | Preclinical | 151 |
| Fluticasone propionate | PLA, PLA-PEG | Mucus-penetrating nanoparticles | It inhibited the accumulation of BALF neutrophils for a longer period of time as compared to the free fluticasone propionate. | Preclinical | 152 | |
| COPD | Fluticasone propionate | Glycerol tripalmitate, glyceryldistearate, CS oligosaccharide lactate | Mucoadhesive solid lipid microparticles | It was more effective than the pure fluticasone propionate in controlling oxidative stress. | Preclinical | 153 |
| Cystic fibrosis | Lumacaftor, ivacaftor | Squalene, PEG, Tween 80, Span 35 | Nanostructured lipid carriers | It showed the superior ability to restore the expression and function of cystic fibrosis transmembrane receptor proteins as compared to the non-encapsulated drugs. | Preclinical | 154 |
| Lung infection | Amikacin | DPPC, cholesterol | Liposomes (Arikace®) | It demonstrated significant activity against Mycobacterium avium complex. | Approved by FDA | 126 |
| Ciprofloxacin | Hydrogenated soy phosphatidylcholine, cholesterol | Liposomes (Pulmaquin®) | It showed antibacterial activity against Pseudomonas aeruginosa. | Phase Ⅲ clinical trails | 155 | |
| Tobramycin | Precirol® ATO 5, Compritol® 888 ATO, Poloxamer 188, Tween 80 | Nanostructured lipid carriers | It exhibited antibacterial potential against isolated Pseudomonas aeruginosa. | Preclinical | 156 | |
| Lung cancer | 9-Nitro-20(S)-camptothecin | Dilauroylphosphatidylc-holine, cholesterol | Liposomes | It was clinically effective in reducing tumor size with minimal toxicity profiles. | Phase Ⅱ clinical trails | 157 |
| Pulmonary hypertension | Bosentan | PLGA, PVA | Polymeric nanoparticles | It exhibited a more persistent vasodilation effect on the pulmonary blood vessels. | Preclinical | 158 |
| Fasudil | DPPC, cholesterol | Liposomes | It provided a sustained vasodilation effect on pulmonary blood vessels. | Preclinical | 159 | |
| Systemic diseases | ||||||
| Bone disorder | Calcitonin | PLGA, PVA, CS | Mucoadhesive polymeric nanospheres | It maintained the blood calcium at low level for a prolonged period of time. | Preclinical | 160 |
| Diabetes | Insulin | CS, mannitol, pentasodium tripolyphosphate | Nanocomposite microparticles | It exhibited a prolonged hypoglycemic effect as compared to the insulin solution. | Preclinical | 161 |
API, active pharmaceutical ingredient; BALF, bronchoalveolar lavage fluid; COPD, chronic obstructive pulmonary diseases; CS, chitosan; DPPC, dipalmitoylphosphatidylcholine; FDA, US Food and Drug Administration; IL-4, interleukin-4; IL-5, interleukin-5; PEG, polyethylene glycol; PLA, polylactic acid; PLGA, poly(lactic-co-glycolic acid); PVA, polyvinyl alcohol.