Table 4.
Type | Drug | Key excipient | Method of preparation | Size | Mode of action | Ref |
---|---|---|---|---|---|---|
Microscale dry powder | A 1,2,4-triazole motif and quinolinone | Lactose | Jet milling | Less than 2 μm | Bifunctional MABAs | [156] |
FP, MF and SX | – |
(1) Jet milling (2) Wet polishing |
(1) 2.18–2.53 μm (2) 0.87–1.49 μm |
Corticosteroids and long-acting β2-agonists | [157] | |
SBS or BD | – |
(1) Jet milling (2) Spray-drying |
(1) 0.59–0.65 μm (2) 0.63–0.69 μm |
Short acting β agonist, synthetic glucocorticoid | [158] | |
dimethyl fumarate | Mannitol | Co-spray dried | 0.56–1.08 μm | Nrf2 activator drug to treat pulmonary inflammation | [159] | |
naringin | Ethanol –water (50:50 v/v) | Co-spray dried | 3.5 µm | Free-radical scavenger drug | [160] | |
Indacaterol and glycopyrronium | – | – | – | Decrease IL-8, IL-10, TNF-α, MMP-9, PON1, increase TIMP-1 and MDA | [161] | |
BD and RES | Ethanol –water (80:20 v/v) | Co-spray dried | 1.0 µm | DECREASE the levels of TNF-α and IL-6 in LPS induce alveolar macrophages | [162] | |
Resveratrol | Ethanol –water (50:50 v/v) | Spray-drying | 3.86 µm | Scavenge activity of more than 50% of DPPH free radicals | [163] | |
Resveratrol | Ethanol–water (50:50 v/v) | Spray-drying | 3.9 μm | The expression of IL-8 from Calu-3 induced with TNF-α, TGF-β1 and LPS were significantly reduced | [164] | |
BD | HA | Spray-drying | 3.12–5.35 μm | Glucocorticoid | [165] | |
Sodium ascorbyl phosphate | HA | co-spray dried | 3.4 µm | ANTI-inflammatory, antioxidant, and wound healing properties | [166, 167] | |
Porous microparticles | Anthocyanin | PLGA microparticles, HA, β-cyclodextrin (porogen); |
W1/O/W2 multi-emulsions freeze drying |
5 ~ 10 μm | Sustain ATH release characteristics and protract antioxidant activity for DPPH radicals | [168, 169] |
BD | PLGA and PVP |
modified single emulsion (O/W) solvent evaporation freeze drying |
6 μm | – | [170] | |
DEX | PVAX |
Double emulsion method freeze drying |
13 μm | Scavenge hydrogen peroxide, diminish oxidative stress | [114] | |
Mucoadhesive solid lipid microparticles | FP | Alginate, chitosan and lipid |
Ethanolic precipitation technique (freeze drying) |
1 ~ 5 μm | ERK1/2 pathway activation | [171] |
SX |
Sodium alginate, Pluronic F68 and lipid |
HPH (freeze drying) |
3.3 μm | Long-acting β2 agonist | [172] | |
NCMPs | NAC |
(1) Phospholipidand, cholesterol; (2) Lactose |
(1) Reverse phase evaporation method (2) Spray drying |
7.2 μm | Against TBARS production | [100] |
MicroRNA | l-Leucine and mannitol |
(1) Oil in water (o/w) single emulsion method; (2) Spray-drying |
4.20 ~ 6.03 µm | Genes silence of IRAK1 and TRAF6 | [122] | |
siRNA |
(1) Lipidoid, PLGA (2) mannitol or trehalose |
(1) DESE (2) Spray-drying |
3.3 µm | Dispersed microembedded LPNs had preserved physicochemical characteristics as well as in vitro siRNA release profile and gene silencing | [173] | |
siRNA |
(1) dendrimer (2) mannitol, trehalose, inulin |
(1) bulk mixing and microfluidics-based mixing (2) spray-drying |
4.8 ~ 5.6 μm | The gene silencing efficiency of the nanocomplexes is preserved upon spray drying | [174] | |
Nanocomposite microparticles (NCMPs) | Curcumin |
(1) PLGA; PEG-g-Cs copolymer or Cs |
(1) Modified single emulsion − solvent evaporation method; (2) Spray-drying |
3.1–3.9 μm | Microparticles have minimal propensity to induce TNF-α release which showed much delayed and reduced macrophage uptake | [175] |
BD |
(1) TPGS (2) Leucine or albumin |
(1) High-energy wet media milling; (2) Spray drying |
4.39 ~ 5.30 μm | Anti-inflammatory activity | [176] | |
Apigenin |
(1) BSA (2) lactose and l-leucine |
(1) Modified nanoparticle albumin-bound technology (2) Spray drying |
2.47 μm | Antioxidant activity of drug is preserved and enhanced by the BSA;, scavenge the DPPH free radial | [177] | |
Clinical study | Ribavirin –PRINT –CFI | 35% ribavirin with 55% trehalose and 10% trileucine | Non-wetting Templates (PRINT) technology | 1 μm | Against the key respiratory viruses that can cause acute exacerbations in COPD | [178] |
Ribavirin-97 PRINT-IP | 1% PVA | Non-wetting Templates (PRINT) technology | 1 μm |
(1) Refers to microparticle or nanoparticle material; (2) refers to matrix materials.
MABAs: muscarinic antagonist and β2 agonist properties; NCMPs: nanocomposite microparticles; Nrf2: dimethyl fumarate activator; MF: mometasone furoate; SX: salmeterol xinafoate; SBS: salbutamol sulphate; BD: budesonide; RES: resveratrol; HA: hyaluronic acid; PON1: Paraoxonase; DPPH: 2,2-diphenyl-1-pikryl-hydrazyl; MDA: Malonyl dialdehyde; HSPB5: Alpha B-crystallin; DEX: Dexamethasone; PVAX: vanillyl alcohol-containing copolyoxalate; HPH: high-pressure homogenization; SX: Salmeterol Xinafoate; TPGS: D-α-tocopherol polyethylene glycol 1000 succinate; BSA: bovine serum albumin