Nanotechnology based drug delivery systems for the treatment of anterior segment eye diseases
Diseases affecting the anterior segment of the eye are the primary causes of vision impairment and blindness globally. Drug administration through the topical ocular route is widely accepted because of its user/patient friendliness – ease of administration and convenience. However, it remains a significant challenge to efficiently deliver drugs to the eye through this route because of various structural and physiological constraints that restrict the distribution of therapeutic molecules into the ocular tissues.
The bioavailability of topically applied ocular medications such as eye drops is typically less than 5%. Developing novel delivery systems to increase the retention time on the ocular surfaces and permeation through the cornea is one of the approaches adopted to boost the bioavailability of topically administered medications. Drug delivery systems based on nanotechnology such as micelles, nanosuspensions, nanoparticles, nanoemulsions, liposomes, dendrimers, niosomes, cubosomes and nanowafers have been investigated as effective alternatives to conventional ocular delivery systems in treating diseases of the anterior segment of the eye.
Highlights
- Topical drug delivery to the eye remains a very challenging area for pharmaceutical scientists
- Nanotechnology-based delivery systems are promising approaches to improve efficiency of topically administered drugs
- There is a strong interest in the use of nano-formulations for delivering phytochemicals to the eye
- Poor scalability of nanoformulations has been reported to be a hindrance to the clinical translation of new products.
This review discussed different nanotechnology-based delivery systems that are currently investigated for treating and managing diseases affecting the anterior ocular tissues. We also looked at the challenges in translating these systems into clinical use and the prospects of nanocarriers as a vehicle for the delivery of phytoactive compounds to the anterior segment of the eye.
Table 1 – Typical active ingredients and excipients used to formulate nanotechnology-based ocular delivery systems
| Drug/Excipients | Examples |
|---|---|
| Active pharmaceutical ingredient | • Anti-inflammatory drugs - dicofenac, pranoprofen, flurbiprofen • Antibacterial - azithromycin, norfloxacin, moxifloxacin, sparfloxacin, ciprofloxacin, gemifloxacin, amikacin, lomefloxacin, vancomycin. • Antifungal - amphotericin B, natamycin, voriconazole • Antiviral - acyclovir, ganciclovir • Immunosuppressant - dexamethasone, cyclosporine A, tacrolimus, tramcinolone • Anti-glaucoma - timolol, carteolol, dorzolamide, acetazolamide, brinzolamide, brimonidine, latanoprost, brimatoprost, travaprost, pilocarpine • Proteins and peptides - lactoferrin, octreotide, catalase, protamine • Genes - transcription factor, plasma DNA, monoclonal, antibody • Phytochemicals - naringenin, resveratrol, hesperetin, glycyrrhizin, curcumin, epigallocatechin gallate and myricetin |
| Polymers | • Natural - chitosan, hyaluronic acid, alginate, albumin, gelatin, gellan gum • Semi-synthetic - sodium carboxymethylcellulose, hydroxypropyl methylcellulose • Synthetic - poly (ethylene glycol), poly(lactic-co-glycolic acid) (PLGA), polycaprolactone (PCL), poly-lactic acid (PLA), poly(glycolic acid) (PGA), polyvinyl alcohol (PVA), poly(acrylic acid) (PAA), methacrylic acid-methyl acrylate copolymer (Eudragit®), poly (amidoamine)(PAMAM), carbosilane |
| Lipids | • Triglycerides - trilaurin, trimyristin, tripalmitin, and tristearin (Dynasan® 112, 114, 116, 118, respectively) • Partial Glyceride - glyceryl tribehenate (Compritol®), polyethylene glycol monosterate (Gelucire®), glyceryl palmitostearate (Precirol®) • Wax - cholesterol • Fatty acid - stearic acid • Amphiphilic lipids - glyceryl monooleate (Capmul®), phytantriol • Liquid lipids - oleic acid, castor oil, squalene, olive oil, coconut oil, palmitic oil, soybean oil, glyceryl tricarylate (Miglyol® 812) • Cationic lipids - 1,2-dioleoyl-3-Trimethylammonium-propane (DOTAP), 1,2-dioleoyl-Sn-glycero-3-phospho- choline (DOPC), cetyl trimethylammonium bromide, stearylamine. • Phospholipids - phosphatidylcholine (PC), phosphatidylglycerol, dipalmitoyl phosphatidylcholine, distearoylphosphatidylcholine (DSPC), dioleoyl phosphatidylcholine (DOPC), 1,2 dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE), 1,2-distearoyl-phosphatidyl ethanolamine-methyl-polyethylene glycol conjugate-2000 (DSPE-MPEG-2000), lecithin |
| Surfactants | • Polysorbate (Tween®), sorbitan esters (Span®), poloxamers (Pluronic®, Lutrol®), tyloxapol, Vitamin E TPGS (D- α -tocopherol polyethylene glycol 1000 succinate), polyoxyl 40 hydrogenated castor oil (Cremophor RH-40), oleylamine, Solutol HS 15® (Kolliphor HS 15®), Transcutol® P • Co-surfactants – propylene glycol, glycerol, ethano |
Following excipients are mentioned in the study besides other: chitosan, hyaluronic acid, alginate, albumin, gelatin, gellan gum, Semi-synthetic – sodium carboxymethylcellulose, hydroxypropyl methylcellulose, Synthetic – poly (ethylene glycol), poly(lactic-co-glycolic acid) (PLGA), polycaprolactone (PCL), polylactic acid (PLA), polyvinyl alcohol (PVA), methacrylic acid-methyl acrylate copolymer (Eudragit®),Triglycerides and tristearin (Dynasan® 112, 114, 116, 118), Partial Glyceride – glyceryl tribehenate (Compritol®), polyethylene glycol monosterate (Gelucire®), glyceryl palmitostearate (Precirol®), Amphiphilic lipids – glyceryl monooleate (Capmul®), castor oil, squalene, olive oil, soybean oil, glyceryl tricarylate (Miglyol® 812), Phospholipids, Polysorbate (Tween®), sorbitan esters (Span®), poloxamers (Pluronic®, Lutrol®), tyloxapol, Vitamin E TPGS (D- α -tocopherol polyethylene glycol 1000 succinate), polyoxyl 40 hydrogenated castor oil (Cremophor RH-40), oleylamine, Solutol HS 15® (Kolliphor HS 15®), Transcutol® P, Co-surfactants – propylene glycol, glycerol, ethanol
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Adaeze Linda Onugwu, Chinekwu Sherridan Nwagwu, Obinna Sabastine Onugwu, Adaeze Chidiebere Echezona, Chinazom Precious Agbo, Stella Amarachi Ihim, Prosper Emeh, Petra Obioma Nnamani, Anthony Amaechi Attama, Vitaliy V. Khutoryanskiy, Nanotechnology based drug delivery systems for the treatment of anterior segment eye diseases, Journal of Controlled Release, Volume 354, 2023, Pages 465-488, ISSN 0168-3659, https://doi.org/10.1016/j.jconrel.2023.01.018.
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