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