Evidences for Anti-Mycobacterium Activities of Lipids and Surfactants

Supplementary file

Evidences for Anti-mycobacterium Activities of Lipids and Surfactants

Afzal Hussaina and Sandeep Kumar Singha

aDepartment of Pharmaceutical Sciences and Technology, Birla Institute of Technology,

Mesra, Ranchi-835215, Jharkhand, India

*Corresponding author:

Dr. Sandeep Kumar Singh, Department of Pharmaceutical sciences and Technology, Birla

Institute of Technology, Mesra, Ranchi-835215, Jharkhand, India,

Mob: +919234653731, Email:[email protected]

1 Supplemental Table T1 Lipids and surfactants with their generic, trade, manufacturer’s name and composition Generic name Trade name Manufacturer Composition Glycerol monocaprylocaprate Capmul MCM ABITEC Corp. Medium chain length mono (60%) and Columbus, OH, USA diglyceride (35%) consisting of 83% w/w caprylic acid (C8) and 17% w/w capric acid (C10). Glyceryl caprylate/caprate Capmul MCM L ABITEC Corp. Glyceryl caprylate/caprate Columbus, OH, USA Glyceryl monocaprylate Capmul MCM ABITEC Corp. Glyceryl monocaprylate; ˃95% C8:0, Columbus, OH, USA 3% C (C8) 10:0 Polyethylene glycol caprylate Capmul PG ABITEC Corp. Polyethylene glycol caprylate Columbus, OH, USA Glycerol dicaprylate NA ABITEC Corp. Medium chain diglyceride (83%) Columbus, OH, USA consisting of 75%-85% caprylic acid (C8). Caprylic/capric triglyceride Captex 355 ABITEC Corp. Medium chain triglyceride consisting Columbus, OH, USA of mixture of caprylic acid (C8) and capric acid (C10) at 55:45 ratio. Macrogolglycerol Ricinoleate Cremophor EL BASF, Tarrytown, NY, The main component (83%) is Ph.Eur.,Polyoxyl 35 Castor Oil USA polyethylene glycol ester of ricinoleic USP acid Polyoxyl Immuno-40 Cremophor BASF, Tarrytown, NY, Polyoxyl immuno-40 hydrogenated hydrogenated castor oil USA castor oil RH40 Labrafac CC Caprylic/capric triglycerides Diethylene glycol monoethyl ether Transcutol P Gattefosse, France Diethylene glycol monoethyl ether Polyethylene glycol 400 PEG 400 Sigma Aldrich Polyethylene glycol 400 Caprylocaproylmacrogolglycerides Labrasol Gattefosse, France Caprylocaproyl polyethylene glycolglycerides Polysorbate 80/polyoxyethylene Tween® 80 Sigma Aldrich Polysorbate 80/polyoxyethylene (20) (20) sorbitan monooleate sorbitan monooleate Lauroyl macroglycerides Gelucires 44/14 Gattefosse, France Lauroyl macroglycerides Propylene Glycol Miglyol® 840 Sasol Propylene glycol Dicaprylate/Dicaprate dicaprylate/Dicaprate Caprylic / Capric/Succinic Miglyol® 829 Sasol Caprylic / Capric/Succinic triglyceride Triglyceride Caprylic / Capric Triglyceride Miglyol® 810 Sasol Caprylic / Capric triglyceride Tricaprylin Miglyol® 808 Sasol Tricaprylin PEG-6, Macrogol 300 Lipoxol 300 PEG-6, Macrogol 300 MED Glycerol monooleate Peceol Gattefosse, France Glycerol monooleate Propylene GlycolDicaprylocaprate Captex 200P ABITEC Propylene glycol dicaprylocaprate Glyceryl Tricaprylate/Tricaprate Captex 300 ABITEC Glyceryl tricaprylate/Tricaprate Glycerol Tricaprylate/Caprate Captex 300EP ABITEC Glycerol tricaprylate/Caprate Propylene glycol monocaprylate Capryol PGMC Gattefosse, France Propylene glycol monocaprylate;

˃90% C8:0 Propylene glycol dicaprylocaprate Labrafac PG Gattefosse, France Propylene glycol dicaprylocaprate Ethoxylated coconut glycerolesters Acconon C 80 ABITEC Ethoxylated coconut glycerol esters

Supplemental Table T2 In vitro anti-mycobacterium activities of lipids, surfactants and co-surfactant against MS-995 and MS-942 Anti-mycobacterium activities of excipients Zone of inhibition (mm) in both strains (mean±sd) S. Excipients MS-995 MS-942 No Oil/lipids

2 1 Capmul PG-8 15.2±1.2 14.5±1.5 2 Capmul MCM 14.0±0.8 9.0±0.7 3 Capmul MCM C8 22.25±0.95 15.5±0.5 4 Capmul MCM L 19.74±1.7 10.75±0.3 5 Miglyol 840 14.25±0.5 13.5±0.5 6 Miglyol 810 13.75±0.9 11.5±1.1 7 Miglyol 829 14.25±0.5 10.25±0.8 8 Miglyol 808 13.75±0.95 12.0±1.2 9 Peceol 12.25±0.9 5.75±1.4 10 Capryol PGMC 14.0±1.0 13.0±1.5 11 Lipoxol 300 MED 9.0±0.6 8.72±1.0 12 Captex 200P 14.25±1.25 11.0±0.8 13 Captex 300 14.25±0.9 9.0±0.7 14 Captex 355 EP 10.0±1.6 11.0±0.5 15 Capryol PGE 860 14.0±1.5 13.0±1.2 16 Almond 12.0±0.5 13.5±1.1 17 Labrafac 11.25±0.8 14.0±0.8 Surfactants and co-surfactants 1 Acconon C-80 16.25±0.5 13.75±1.6 2 Labrasol 17.25±0.5 18.0±2.0 3 Cremophor EL 0 0 4 Cremophor RH 40 0 0 5 Transcutol P 0 0 6 Tween® 20 0 0 7 Tween® 40 13.25±0.9 12.0±0.2 8 Tween® 60 12.5±1.0 15.25±0.5 9 Tween® 80 12.75±1.2 10.25±0.5 10 Sodium cholate 16.3±1.2 11.5±0.57 11 Sodium deoxycholate 15.75±1.7 13.25±4.0 12 Sodiun tauroglycholate 14.0±0.8 11.5±1.2 13 Gelucire 44/14 14.0±1.2 13.5±0.5 14 PEG 400 14.8±1.3 11.0±0.82 15 SoluPlus 0 0 16 Solutol-HS 15 0 0

Supplemental Table T3 Minimum inhibitory concentration of selected excipient against the Mycobacterium smegmatis (MS-995 and MS-942) Excipients Minimum inhibitory concentration (MIC) value (mg/ml) MS-995 MS-942 Labrasol 25.0± 1.0 25.0±1.0 Capmul MCM C- 12.5±0.5 18.75±0.8 8

3 Acconon C-80 12.5±0.5 15.625±2.5

Supplementary Figure S1

4 100

80 ) % (

60 s i s y l o m e 40 H

Figure S1 Bar graph of percent hemolysis in presence of excipients over period of 24 hrs