Table 1.
References (Year) | Drug | Drug Concentration (%) a | Stabilizer(s) b | Stabilizer Concentration (%) a | Reported Smallest Median or Mean Particle Size after Milling (nm) |
---|---|---|---|---|---|
Bitterlich et al. (2015) [73] | Naproxen | 5 | Poloxamer-188, PVP-K 30, PVA-Mowiol 3-85, Mowiol 4-88, PVP-VA64, HPC-LF, Polysorbate-80, TPGS, SDS, HPMC | 0.1–15 | ~150 |
Dong et al. (2015) [74] | SNX-2112 | 1 | Poloxamer-188, Polysorbate-80 | 0.01–1 | 203 |
Kumar et al. (2015) [75] | Danazol | 1 | PVP-K 30, 40, PVA, HPMC-E3, E5, E15, Methocel-A15, SDS, TPGS, Poloxamer-188, 407, Dowfax-2A1, HPC | 0.2 | 168 |
Afolabi et al. (2014) [45] | Griseofulvin | 5–30 c | HPC-SL | 2.5 | 132 |
SDS | 0.5 | ||||
Bhakay et al. (2014) [76] | Griseofulvin, Azodicarbonamide | 10 c | HPC-SL, SDS | 0–2.5 | 160 |
Bitterlich et al. (2014) [59] | Cinnarizine, Fenofibrate | 10 | DOSS | 0.25 | 276 |
SDS | 0.1 | ||||
Poloxamer-188, PVP-K30, PVP-VA64, PVA-Mowiol 3–85, Polysorbate-80, HPMC, Vit-E TPGS | 2.5 | ||||
Komasaka et al. (2014) [77] | Cilostazol, Curucumin, Furosemide, Naproxen, Phenytoin, Nifedipine, Danazol, Spironolactone, Cinnarizine, Piroxicam, Indomethacin | 10, 20 | HPMC of different molecular weight, TC-5E, MC-400, Metolose, PVP-K17, Polysorbate-80, SDS, Cremophor-RH40, Poloxamer-188, Vit-E TPGS | 0.5 | ~120 |
Leng et al. (2014) [78] | Paliperidone palmitate | 15 | Polysorbate-80 | NM f | 492 (±8) |
Mahesh et al. (2014) [79] | Glipizide | 1.6 | SDS, Poloxamer-188, 407, Polysorbate-80 | 2.5–7.5 d | NM f |
PVP-K30, HPMC | 2.5–5 d | ||||
Shah et al. (2014) [80] | Glibenclamide | 0.5 | PVP-S630 D, Poloxamer-188, Polysorbate-80, HPMC, HPC, HEC, SDS | 0.25 | 329 |
Sarnes et al. (2014) [81] | Itraconazole | 15 | Poloxamer-407 | 9–12 | 315 (±5) |
Yuminoki et al. (2014) [82] | Griseofulvin, Hydrochlorothiazide, Tolbutamide, Acyclovir, Indomethacin, Diprydamole, Naproxen, Piroxicam, Phenytoin | 1–20 | HPC, PVP, POVA, PVA | 1–10 | 120 (±2) |
Bhakay et al. (2013) [58] | Griseofulvin, Phenylbutazone | 10 c | HPC-SL, SDS | 0–2.5 | 145 |
Mannitol | 10 | ||||
Cerdeira et al. (2013) [83] | Miconazole, Itraconazole | 5–20 | SDS | 0–0.2 | 136 |
HPC-LF | 1.25–5 | ||||
HPMC-E15, Poloxamer-188, 407 | 5 | ||||
George and Ghosh (2013) [84] | Naproxen, compound A, B, C, D and E from Novartis | 5 | Vit-E TPGS, Poloxamer-407, SDS, DOSS | 1 | <500 |
HPMC | 2.5 | ||||
Knieke et al. (2013) [64] | Fenofibrate | 2.5 | HPMC-E3 | 5–50 e | 151 |
SDS | 5–20 e | ||||
Monteiro et al. (2013) [85] | Griseofulvin, Naproxen | 10 c | HPC-SL | 2.5 | 138 |
SDS | 0.0825, 0.5 | ||||
Niwa and Danjo (2013) [86] | Phenytoin | 8 | PVP-K30 | 0.25–16 | 168 |
SDS | 0.1 | ||||
Ghosh et al. (2012) [47] | NVS-102 | 2, 5 | HPMC | 1 | 277 |
Vit-E TPGS | 0.5–5 | ||||
Tanaka et al. (2012) [6] | Probucol | 1 | Gelucire-44/14, Gelucire-50/13, Vit-E TPGS, Poloxamer-188, 338 | 1 | 77 |
Sievens-Figueroa et al. (2012) [36] | Naproxen, Fenofibrate, Griseofulvin | 10c | HPMC-E15LV | 2.5 c | 144 |
SDS | 0.075, 0.5c | ||||
Ali et al. (2011) [87] | Hydrocortisone | 2 | PVP, Polysorbate-80 | 0.2 | 300 |
HPMC | 0.5 | ||||
Bhakay et al. (2011) [65] | Itraconazole, Fenofibrate, Griseofulvin, Ibuprofen, Azodicarbonamide, Sulfamethoxazole | 2c | SA, SDS, HPMC, Polysorbate-80 | 0.1 | 740 |
HPMC-E15 LV | 0.2 | ||||
Cerdeira et al. (2011) [46] | Miconazole, Itraconazole, Etravirine | 20 | HPC-LF | 5 | 129 |
SDS | 0–0.2 | ||||
Chin et al. (2011) [62] | Carbofuran | 40.6, 44 | Atlox-4913 | 4–7 | 29 |
PVP-K30 | 1–3 | ||||
Miglyol-812 | 1–3 | ||||
Ghosh et al. (2011) [88] | Compound NVS-102 | 5 | Vit-E TPGS | 3, 5 | 230.2 |
SDS, HPMC, PVP-K30 | 1 | ||||
Poloxamer-188, 407 | 2 | ||||
Liu et al. (2011) [89] | Indomethacin, Itraconazole | 40 | Polysorbate-80, PEG-6000, Poloxamer-188, 407 | 10–80 e | 345 |
Cerdeira et al. (2010) [57] | Miconazole | 5–25 | HPC-LF | 1.25–6.25 | 140 |
HPC-EF, PVP-30, Poloxamer-188, HPMC-E15 | 1.25, 2.5 | ||||
SDS | 0.0125, 0.05, 0.2 | ||||
DOSS (SD) | 0.1, 5 | ||||
BKC | 0.1 | ||||
Juhnke et al. (2010) [63] | Naproxen | 2 | HPC-LF | 0.5 | 151 |
Compounds A and B, from Novartis | |||||
Patel et al. (2010) [90] | Famotidine | 0.4 | HPMC-K15M, PVP-K30, Polysorbate-80, Poloxamer-188, 407 | 0.4, 0.8 | 244.6 |
Baert et al. (2009) [91] | Rilpivirine (TMC278) | 12.5 | Poloxamer-338 | 3.125 | 200 |
Vit-E TPGS | 3.125 | ||||
Fakes et al. (2009) [92] | HIV-attachment inhibitor: BMS-488043 | 10 | HPC-SL | 1.25, 2.1 | 120 |
SDS, DOSS | 0.1 | ||||
Tanaka et al. (2009) [93] | Omeprazole, Albendazole, Danazol | 1 | Polysorbate-80, Poloxamer-188, 407 | 0.05–5 | 102 |
Van Eerdenbrugh et al. (2009) [94] | Loviride, Itraconazole, Cinnarizine, Griseofulvin, Indomethacin, Mebendazole, Naproxen, Phenylbutazone, Phenytoin | 20 | PVP-K30, K90, PVA-PEG (K-IR), Poloxamer-188, Vit-E TPGS, PVA, Polysorbate-80 | 10–100 | >1000 |
HPMC-E15, HEC, HPC, MC, NaCMC, NaAlg | 1–10 | ||||
Ain-Ai and Gupta (2008) [95] | Naproxen | 10, 30 | HPC | 1–4 | 417 |
AH | 0–1.2 | ||||
Choi et al. (2008) [96] | Itraconazole | 8 | HPC of different molecular weights | 1.33 | 110 |
Deng et al. (2008) [97] | Compound A | 15 | Plasdone S-630 | 3.5, 4.1 | 82 |
SD | 0.25, 0.295 | ||||
Lee et al. (2008) [98] | Ibuprofen, Glimepiride, Digitoxin, Naproxen, Biphenyl dimethyl dicarboxylate, Paclitaxel, Lipoic acid, Predinisolone acetate, Nifedipin, Hydrocortihydrocortisone acetate, Itraconazole | 8 | HPC, PVP, PEG , Poloxamer-188, 407 | 1.33 | 119 (±37) |
SDS, Benzethonium chloride | 1 | ||||
Van Eerdenbrugh et al. (2008) [23] | Loviride, Itraconazole, Cinnarizine, Griseofulvin, Indomethacin, Mebendazole, Naproxen, Phenylbutazone, Phenytoin | 20c | Vit-E TPGS | 25 e | 156 |
Dai et al. (2007) [99] | Poorly water soluble compound/carrageenan complex | 5 | Poloxamer-407 | 0.75 | 300 |
Tyloxapol, HPMC-2910, HPC-SL | 1.5, 2 | ||||
PVP-K30 | 0.75, 2 | ||||
Plasdone-S630 | 1.31, 2 | ||||
DOSS | 0.15 | ||||
Sepassi et al.(2007) [100] | Nabumetone, Halofantrine | 20 | HPMC-E3LV, E4M, PVP-K12, K30, K90 | 0.63–6.25 | 650 |
Van Eerdenbrugh et al.(2007) [101] | Loviride | 20 | Polysorbate-80, Poloxamer-188 | 50 e | 264 (±14) |
Jinno et al. (2006) [102] | Cilostazol | 0.25 | HPC | 16.5 | 220 |
DOSS | 0.8 |
a With respect to suspension, w/v or w/w; b Names of the stabilizers are abbreviated: AH: Arginine hydrochloride; Atlox 4913: Poly(methyl methacrylate) poly(ethylene glycol) graft copolymer; BKC: Benzalkonium chloride; DOSS (SD): Dioctyl sulfosuccinate sodium salt (sodium docusate); HEC: Hydroxyethylcellulose; HPC: Hydroxypropyl cellulose; HPMC: Hydroxypropylmethyl cellulose; MC: Methylcellulose; Miglyol 812: a 60/40 (w/w) mixture of C8 and C10 triglycerides; NaAlg: Alginic acid sodium salt; NaCMC: Carboxymethylcellulose sodium salt; PEG: Polyethylene glycol; Plasdone S-630: Copoviodone, Vinyl pyrrolidone/vinyl acetate copolymer; PVA: Polyvinyl alcohol; PVA-PEG: Polyvinyl alcohol polyethylene glycol graft copolymer; PVP: Polyvinylpyrrolidone; SDS: Sodium dodecyl sulfate; SA: Sodium alginate; Vit-E TPGS: d-alpha tocopheryl polyethylene glycol 1000 succinate; POVA: PVA copolymer with grafted poly acrylic acid and poly methyl methacrylate (PMMA) groups; c with respect to deionized water; d stabilizer:drug; e with respect to drug weight; f not mentioned.