Table 3.
Active molecules incorporated in transfersomes and other deformable liposomes investigated for dermal/transdermal administration: in vitro, in vivo preclinical and clinical studies (presented in chronological order).
| Active Molecule | Molecular Weight (g/mol) | Log p | Indication | Study | Ref. |
|---|---|---|---|---|---|
| Human serum albumin Gap junction proteins |
66430.0 N/A |
N/A N/A |
Immunogenic proteins | In vivo effect on inducing antigen-specific antibodies in mice | [50] |
| Insulin | 5734 | N/A | Anti-diabetic | In vivo measurement of hypoglycemic effect in mice and healthy human volunteers | [49] |
| Diclofenac sodium | 318.1 | 0.7 1 | Anti-inflammatory | In vitro permeation and drug deposition studies on rat skin; in vivo deposition in target tissues studies on mice, rats and pigs | [101,115] |
| Triamcinolone acetonide | 434.5 | 2.53 1 | Anti-inflammatory | In vivo localization in mice skin; in vivo bioactivity murine ear edema; double-blind, placebo-controlled clinical trial on healthy volunteers | [116,117] |
| Hydrocortisone | 362.46 | 1.6 1 | Steroidal anti-inflammatory | In vivo evaluation of the anti-inflammatory effect in mice with arachidonic induced edema | 51] |
| Dexamethasone | 392.46 | 1.8 1 | Steroidal anti-inflammatory | In vivo evaluation of the anti-inflammatory effect in mice with arachidonic induced edema | [51] |
| Methotrexate | 454.44 | 1.85 2 | Anti-cancer | In vitro permeation and deposition study on pig ear skin | [38] |
| Ketotifen fumarate | 425.5 | 3.3 3 | Anti-histaminic | In vitro permeation and skin deposition study on rabbit pinna skin | [76,77] |
| Meloxicam | 351.4 | 3.43 1 | Anti-inflammatory | In vitro permeation study on shed snake skin from the Siamese cobra | [118] |
| Ketoconazole | 531.43 | 4.3 4 | Antifungal | In vitro drug release across cellulose membranes and permeation study on pig skin | [119] |
| Terbinafine | 291.43 | 5.51 3 | Antifungal | In vitro measurement of anti-fungal effect against Dermatophyte Hyphae in samples from a clinical study. | [120] |
| Sertraline | 306.23 | 5.06 3 | Anti-depressant | In vitro drug release study on cellophane membrane; in vitro drug permeation through rat skin; in vivo evaluation of the antidepressant activity using forced swim model test | [121] |
| Linoleic Acid | 280.44 | 7.06 1 | Skin whitening | In vitro percutaneous permeation through human stratum corneum and viable epidermis membrane | [83] |
| Itraconazole | 705.64 | 5.66 1 | Anti-fungal | In vitro penetration and permeation study on rat skin | [54] |
| Ketoprofen | 254.3 | 3.1 1 | Treatment of osteoarthritis | Randomized clinical study conducted on knee osteoarthritis patients | [122] |
| Lycopene | 536.87 | 9.6 3 | Anti-inflammatory | In vitro skin permeation and skin retention study; in vivo tests on anthralin-induced ear swelling in mice | [88] |
| Cisplatin Imiquimod |
300 240.3 |
−2.19 2 2.7 2 |
Treatment of cutaneous epithelial malignancy | In vivo skin localization and biodistribution in mice; in vivo evaluation of dermal, hepato- and nephro-toxicity in mice and rats | [123] |
| Cinnamic acid | 148.16 | 2.1 1 | Antioxidant and anti-inflammatory | In vivo micro-dialysis study in rats | [124] |
| Felodipine | 384.26 | 3.90 1 | Anti- hypertensive | In vitro deposition and permeation study on rat skin | [125] |
| Tetanus toxoid | 6400 | N/A | Tetanus vaccine | In vivo evaluation of protection against tetanus toxin challenge in mice | [62] |
| Raloxifene hydrochloride | 510 | 5.45 3 | Treatment of invasive breast cancer | In vitro release through dialysis membrane; in vitro permeation though rat skin; in vitro permeation and deposition study on rat skin | [126,127] |
| Sildenafil | 474.58 | 2.75 1 | Erectile dysfunction | In vitro permeation through synthetic nylon membrane | [128] |
| Ginsenoside Rh1 | 638.9 | 4.3 4 | Anti-allergic and anti-inflammatory | In vitro skin permeation study on human cadaver skin | [94] |
| Cytarabine | 243.22 | −2.8 2 | Treatment of leukemia | In vitro permeation and deposition study on rat skin. | [129] |
| Pentoxifylline | 278.31 | 0.29 2 | Treatment of intermittent claudication and chronic occlusive arterial diseases | In vitro drug release using dialysis bags | [130] |
| Timolol maleate | 316.42 | 1.44 3 | Anti-hypertensive | In vitro permeation study through synthetic cellulose nitrate membranes; in vitro permeation study using shaved rat skin; in vivo pharmacokinetic study in rats | [131,132] |
| Eprosartan mesylate | 520.6 | 3.57 3 | Anti- hypertensive | In vitro permeation through rat skin; in vivo anti-hypertensive effect on rats with methyl prednisolone acetate-induced hypertension | [133] |
| Tocopherol | 430.71 | 8.84 3 | Skin regeneration | In vitro studies on human keratinocytes cells and fibroblasts; cell viability and antioxidant activity | [134] |
| Ondansetron | 329.82 | 2.4 1 | Management nausea and vomiting | In vitro permeation study on rat skin | [135] |
| Minoxidil and Caffeine | 209.25 149.25 |
3.32 1 −0.1 4 |
Treatment of alopecia | In vivo effect on hair growth | [52] |
| Resveratrol | 228.25 | 2.57 3 | Antioxidant | In vitro transdermal delivery analysis using the Strat-M® Membrane (Merck, Darmstadt, Germany) | [136] |
| Human Growth Hormone | 848.9 | N/A | Hormone replacement therapy | In vitro penetration and permeation studies through rat skin; in vitro skin permeation and biological activity. | [137,138] |
| Lidocaine base | 234.34 | 2.3 3 | Local Anesthetic | In vitro release study through dialysis cellulose membrane | [139] |
| Adapalene | 412.52 | 6.92 3 | Treatment of acne vulgaris | In vitro penetration and permeation study using goat skin membrane; in vivo effect on mice with testosterone-induced acne | [140] |
| Retinyl palmitate | 524.86 | 10.12 3 | Skin regeneration | In vitro skin penetration and fluorescent biodistribution assays on pig ear skin | [141] |