The Use of Polymer Blends in the Treatment of Ocular Diseases
The eye is an organ with limited drug access due to its anatomical and physiological barriers, and the usual forms of ocular administration are limited in terms of drug penetration, residence time, and bioavailability, as well as low patient compliance. Hence, therapeutic innovations in new drug delivery systems (DDS) have been widely explored since they show numerous advantages over conventional methods, besides delivering the content to the eye without interfering with its normal functioning. Polymers are usually used in DDS and many of them are applicable to ophthalmic use, especially biodegradable ones. Even so, it can be a hard task to find a singular polymer with all the desirable properties to deliver the best performance, and combining two or more polymers in a blend has proven to be more convenient, efficient, and cost-effective. This review was carried out to assess the use of polymer blends as DDS. The search conducted in the databases of Pubmed and Scopus for specific terms revealed that although the physical combination of polymers is largely applied, the term polymer blend still has low compliance.
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Polymer blends found from the search for polymeric drug delivery systems for ophthalmic use
(in the databases Pubmed and Scopus)
| Target | Drugs | Polymers | Technology | Administration |
|---|---|---|---|---|
| Corneal wound healing | Ferulic acid | Pluronic® F68 and hyaluronan | Nanocomposite (micelle-nanogel) | Topical (ocular) |
| Infectious ocular keratitis | hLF 1-11 (synthetic antimicrobial peptide derived from human lactoferrin) | Hydroxypropylmethylcellulose (HPMC) and HA | Freeze-dried ocular insert | Topical (ocular)—no in vivo tests |
| Subconjunctival retention | Sunitinib malate | Methylcellulose (MC), HA and PLGA | Microparticles | Subconjunctival injection |
| Ocular hypertension | Dorzolamide HCl | Chitosan, PCL, and PVA | Polymeric nanoparticles | Topical (ocular) |
| Cornal permeability | Myricetin | Polyvinyl caprolactam, polyvinyl acetate, and polyethylene glycol graft copolymer | Polymeric micelles | Topical (ocular) |
| Fungal keratitis | Amphotericin B | PVA and PVP | Microneedle ocular patch (polymer composite) | Micromolding technique to mimic contact lenses |
| Steroid-induced cataract | Triamcinolone acetonide | PLC and Pluronic® F68 | Polymeric core-shell nanoparticles | Topical (eye drops) |
| Ocular hypertension | Timolol maleate | HPMC and HA | Composite ocular films | Topical (eye drops) |
| Increase hydrophobic drugs penetration | Tacrolimus | Amino-terminated poly(ethylene glycol-block-poly(D,L)-lactic acid) (NH2-PEG-b-PLA) and HPMC | Nanomicelles | Topical (eye drops) |
| Bacterial Keratitis | Ofloxacin | Chitosan and PEG | Enhanced lipid nanoparticles | Topical (eye drops) |
| Corneal neovascularization | Axitinib | MPEG and PCL | Polymeric micelles | Topical (ocular) |
| Ocular hypertension | Dorzolamide HCl | Carbopol and HPCM | pH-triggered in situ gel (ISG) | Topical (ocular) |
| Dry eye disorders and corneal ulcer | Levofloxacin | HPMC and sodium alginate | pH-triggered in situ gel (ISG) | Topical (ocular) |
| Ocular drug delivery | Azelastine HCl | Pluronic® F127 and carbopol | Polymeric micellar gel | Topical (eye drops) |
| Ocular drug delivery | Levofloxacin | Eudragit® RS and carbopol | Mucoadhesive minitablets | Topical (ocular) |
| Ocular drug delivery | Triamcinolone acetonide | α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide (PHEA), and poly-butylene succinate (PBS) | Microfibrillar polymeric ocular inserts | Topical (ocular) |
| Ocular drug delivery | Small peptides | Polyoxyethylene hydrogenated castor oil 40 (HCO-40) and octoxynol 40 (OC-40) | Self-assembling multi-layered nanomicelles | Topical (ocular) |
| Glaucoma | Timolol maleate | Chitosan, PVP, and poly (N-isopropylacrylamide) | Ocular contact lenses | Topical (ocular) |
| Fungal keratitis | Econazole | Carboxymethyl-α-cyclodextrin and chitosan | Eye drops | Topical (ocular) |
| Anterior segment of the eye | Betaxol hydrochloride | Cellulose acetate and Eudragit S100 | Inner layer-embedded contact lenses | Topical (ocular) |
| Anterior segment of the eye | Diclofenac sodium | Ethyl cellulose and Eudragit S100 | Inner layer-embedded contact lenses | Topical (ocular) |
| Controlled release of poorly bioavailable drugs into the aqueous humor | Cannabigerolic acid | Hydrogel: Methylcellulose (MC) and HAnanoparticles: poly(ethylene oxide) and PLA | In-situ forming nanoparticle-laden hydrogel | Topical (ocular) |
| Ocular hypertension | Timolol maleate | Chitosan and gelatin | Hydrogel | Topical (ocular) |
| Bacterial growth | Moxifloxacin hydrochloride, chlorhexidine diacetate monohydrate, and diclofenac sodium salt | Sodium alginate, HA, chitosan, and polylysine hydrobromide | Layer-by-layer coatings on contact lenses (hydrogel) | Topical (ocular) |
| Dry eye syndrome | Cyclosporine A | PEG and PLA | Polymeric micelles | Topical (ocular) |
| Glaucoma | Timolol (precursor) | PEG and polyamidoamine (PAMAM) | Polymeric dendrimer | Topical (ocular) |
| Autoimmune uveitis | Cyclosporine A | Methoxy-poly(ethylene-glycol)-hexyl substituted poly-(lactic acid) (mPEGhexPLA) | Nanocarriers | Topical (ocular) |
| Keratoprosthesis, orthokeratology, and mini-scleral lens | - | Ester-based polyurethane (EBPU), N,N-dimethylacrylamide (NNDMA), N-vinyl pyrrolidone (NVP), and acryloylmorpholine (AMO) | High modulus hydrogels | Topical (ocular) |
| Hyperacute bacterial conjunctivitis and endophthalmitis | Tobramycin sulfate | Chitosan HCl and Poloxamer 407 | Mucoadhesive microparticles incorporated in thermosensitive in situ gel | Topical (ocular) |
| Glaucoma | Acetazolamide | HA and PEG | Polymeric films | Topical (ocular) |
| Corneal keratitis or bacterial endophthalmitis | Moxifloxacin | HPMC, PVP-K30, and PEG | Ocular inserts | Topical (ocular) |
| Bacterial keratitis | Ceftazidime | Chitosan, HPMC, and HA | Mucoadhesive nanoparticles | Topical (eye drops) |
| Corneal delivery | Besifloxacin | PVA and PVP | Polymeric microneedles | Topical (ocular) |
| Anterior segment of the eye | Curcumin | PVCL, PVA, and PEG | Polymeric nanomicelles | Topical (ocular) |
| Glaucoma | Resveratrol | PEG and chitosan | Polymeric nanoparticles | Topical (ocular) |
| Glaucoma | - | Poly(N-isopropylacrylamide) and gelatin | Hydrogel | Intracameral injection |
| Dry eye syndrome | Epigallocatechin gallate | Gelatin-gpoly(N-isopropylacrylamide) | In situ gelling carriers | Topical (ocular) |
| Fungal keratitis | Amphotericin B | Chitosan and Poloxamer® 188 | Nanostructured lipid carriers | Topical (ocular) |
| Glaucoma | Acetazolamide | Ethyl cellulose and Eudragit RS100 | Polymeric nanocapsules | Topical (ocular) |
| Glaucoma | Pilocarpine hydrochloride | Gelatin-gpoly(N-isopropylacrylamide) | In situ forming hydrogel | Intracameral injection |
| Retinal diseases | Erythropoietin | Chitosan and hyaluronic acid (HA) | Nanoparticles | Topical (ocular) |
| Systemic absorption and brain-targeting effect | Vinpocetine | Carbopol and HPCM | pH-triggered in situ gel (ISG) | Topical (ocular) |
| Treatment of mid-posterior diseases. | Glycylsarcosine | Chitosan-glutathione | Functional intercalated nanocomposites | Topical (ocular) |
| Proliferative vitreoretinopathy | Ibuprofen and all-trans retinoic acid | Dimethylsiloxiane, PEG, and silicone | Polymer grafts | - |
| Delivery to ocular tissues | - | Polysaccharides | In situ forming gel | Topical (ocular) |
| Ocular drug delivery | - | - | Liposomes, SLN, NLC, niosomes... | Ocular |
| Ocular drug delivery | - | - | Contact lenses | Topical (ocular) |
| Ocular drug delivery | - | - | Polymeric nanomicelles | Topical (ocular) |
| Ocular drug delivery | - | - | Contact lenses | Topical (ocular) |
| Improve drug delivery and encapsulation in nanocarriers | - | Chitosan, PLGA, alginate | Nanoparticles | Topical (ocular) |
| Improve drug delivery and residence time | - | Gellan gum and Pullulan | Electrospun nanofibers | Topical (ocular) |
| Bacteria and fungi ocular infections | - | Two antibacterial synthetic polymers with dipyridine motif | ? | Topical (ocular) |
| Ocular drug/gene delivery | - | PLGA, chitosan and gelatin | Nanocarriers | Ocular |
| Ocular drug delivery | - | - | Micro and nanoparticles (gels) | Topical (ocular) |
| Drug delivery | Triamcinolone acetonide and ovoalbumin | PEG and diacrylate (PEGDA) | Implants | - |
| Oncology and ophthalmology | - | - | Molecularly imprinted polymers (MIP) | - |
| Ocular inflammation | Tacrolimus | PEG2000 and derivatives | Polymeric micelles | Topical (ocular) |
| Ocular drug delivery | Dexamethasone sodium phosphate | Poloxamer 188 and Poloxamer 407 | In situ gel loaded with nanoparticles | Topical (ocular) |
| Sustained delivery of macromolecules | Insulin, catalase, octreotide, IgG, IgG Fab, Lysozyme, BSA | P(CL-co-GA)-PEG-P(GA-co-CL) | Polymeric nanoparticles | Ocular |
| Neovascular ocular diseases | Imatinib | HA and PEG | Polymeric micelles | Topical (ocular) |
| Ocular drug delivery | Infliximab | HA, N-isopropylacylamide (pNIPAAM) and PEG | Collapsible hyaluronic acid hydrogels | Intraocular injection |
| Ocular inflammatory disorders | Pioglitazone | PLGA and PEG | Polymeric nanospheres | Topical (ocular) |
| Ocular drug delivery | Timolol maleate, dexamethasone, and dorzolamide hydrochloride | Poloxamer 407, Poloxamer 188, and chitosan | In situ forming ophthalmic gel | Topical (eye drops) |
| Ocular drug delivery | Pilocarpine hydrochloride | Cellulose and Poloxamer 407 | In situ gelling thermo-responsive hydrogels | Topical (ocular) |
| Intraocular inflammation | Moxifloxacin hydrochloride | Chitosan and HA | Lipid-polymer hybrid nanoparticles | Topical (ocular) |
| Ocular drug delivery | - | - | Polymeric micelles | Ocular |
| Ocular drug delivery | - | - | Lens-based and conventional drug delivery | Topical (ocular) |
| Choroidal neovascularization | Cell-penetrating peptides | PEG and PLGA | Polymeric nanoparticles | Topical (ocular) |
| Ocular drug delivery | Vancomycin | Eudragit® RS100 and carbopol | Polymeric nanoparticles | Topical (ocular) |
| Ocular drug delivery | Pilocarpine hydrochloride | Poloxamer 407 and gellan gum | In situ gelling systems | Topical (ocular) |
| Ocular drug delivery | Flurbiprofen | PCL and poloxamer 188 | Freeze-dried polymeric nanoparticles | Topical (eye drops) |
| Delivery to ocular tissues | - | - | Contact lenses | Topical (ocular) |
| Ocular drug delivery | - | - | Dendrimers | - |
| Ocular drug delivery | - | Elastin-like polypeptides | - | - |
| Ocular inflammation and infection | Dexamethasone sodium phosphate and Tobramycin sulfate | Poloxamer 407 and HPMC K4M | Thermoresponsive ophthalmic in situ gel | Topical (ocular) |
| Ocular drug delivery | Fluorescein sodium and ofloxacin | Pluronic® F127 and Pluronic® F68 | In situ gelling system | Topical (ocular) |
| Ocular drug delivery | Lidocaine | PLGA and collagen | Polymeric nanoparticles | Topical (ocular) |
| Ocular drug delivery | Diclofenac sodium | Methoxy PEG-PCL copolymers and α-cyclodextrin | Micellar supramolecular hydrogel | Topical (ocular) |
| Ocular drug delivery | - | - | Polymeric microsponges | Topical (ocular) |
Author information:
Arribada, R.G.; Behar-Cohen, F.; de Barros, A.L.B.; Silva-Cunha, A. The Use of Polymer Blends in the Treatment of Ocular Diseases. Pharmaceutics 2022, 14, 1431. https://doi.org/10.3390/pharmaceutics14071431