Colloidal drug delivery system: amplify the ocular delivery

Figures & data

Figure 1. Different ocular barriers of topical drug delivery.

Figure 2. Systemic representation of drug disposition model in the eye after topical instillation.

Table 1. Colloidal approaches of various drugs for ocular delivery.

Drug	Polymer	Formulation	Result	References
Everolimus	Oil	ME	Stable, 8.64 ng/ml reached 30 min	Baspinar et al. (2008)
Pilocarpine	Oil	ME	Decreased IOP by 25%	Garty et al. (1994)
Dexamethasone	Oil	CS MEs	Enhance bioavailability	Kesavan et al. (2013)
Vitamin A palmitate	Oil	MEs	Provided better wettability and longer ocular retention	Ma et al. (2008)
Chloramphenicol	Oil	MEs	Tamibility increases remarkably than eye drop	Lv et al. (2005)
Dexamethasone	Oil	MEs	AUC two-fold higher than conventional	Fialho & da Silva-Cunha (2004)
Timolol	Oil	MEs	AUC 3.5-fold than timolol eye drop in aqueous humor	Gasco et al., 1989
Betoxalol	CS	NPs	Marked reduction in IOP	Jain et al. (2013)
Cyclosporine	CS	NPs	Enhanced residence time at the corneal and conjunctival surfaces	Başaran et al. (2013)
Dorzolamide hydrochloride or timolol maleate	HS + CS	NPs	Produced a marked decrease in IOP	Wadhwa et al. (2010)
5-FU	CS	NPs	Bioavailability NPs was significantly higher than 5-FU solution in aqueous humor of rabbit eye	Nagarwal et al. (2011)
Dorzolamide HCl and pramipexole HCl	CS	NPs	Show good mucoadhesion and in vitro release	Papadimitriou et al. (2008)
LCS-NP complex	CS	NPs	No cytotoxicity on conjunctival epithelial cell line IOBA-NHC and strong cellular uptake by corneal epithelium	Diebold et al. (2007)
Cyclosporine	CS	NPs	Prolonged control release cyclosporine to the cornea and conjunctiva in rabbit	Campos et al. (2001)
Metipranolol	CS	NPs	Decreases the systemic side effect	Losa et al. (1993)
5-Fluorouracil (5-FU)	Sodium alginate–CS	NPs	Bioavailability NPs was significantly higher than 5-FU solution in aqueous humor of rabbit eye	Nagarwal et al. (2012)
Indomethacin	Poly(ε-caprolactone (PECL)	Nanocapsules, NPs	Enhance the corneal penetration and ocular bioavailability in rabbit eye	Calvo et al. (1996)
Ganciclovir	Albumin	NPs	Sustained release of ganciclovir over a days	Merodio et al. (2002)
Ganciclovir	Albumin	NPs	Increased antiviral activity against human cytomegalovirus infection	Irache et al. (2005)
Pilocarpine	Albumin	NPs	Increased the bioavailability of pilocarpine by ∼50–90% (miosis), and 50–70% of IOP, respectively, compared to a pilocarpine solution	Zimmer et al. (1994)
Melatonin	PLGA	NPs	Produced a marked decrease in IOP	Musumeci et al. (2013)
Brimonidine and timolol maleate	PLGA	Hybrid hydrogel dendrimer	Effective IOP reduction over days	Yang et al. (2012)
Sparflaxacin	PLGA	NPs	Enhanced residence time and bioavailability in rabbit eye	Gupta et al. (2010)
Levofloxacine	PLGA	NPs	Enhanced residence time and bioavailability in rabbit eye	Gupta et al. (2011)
Flurbiprofen	PLGA nanospheres	Nanospheres	Enhanced the corneal permeation ex vivo	Vega et al. (2008)
Flurbiprofen	PLGA	NPs	Significant anti-inflammatory efficacy	Vega et al. (2006)
Carteolol	Polyalkylcyanoacrylate	NPs and Nanocapsules	Decrease in IOP was much more pronounced with carteolol incorporated into the colloidal carriers than with the commercial eye drops.	Heussler et al., 1993
Metipranolol	Poly-isobutylcyanoacrylate PBCA/PECL	Nanocapsules	10% reduction in IOP in 6 h	Losa et al. (1993)
Indomethacin and cyclosporine	PECL	Nanospheres	Five times superior corneal absorption than oily solution	Alonso et al. (1995)
Minocycline	Lipid	Liposomes	Enhance the therapeutic efficacy in retina after a subconjunctival injection	Kaiser et al. (2013)
Tacrolimus	Bile salts + lipid	Liposomes	3–4-fold higher cellular uptake than conventional liposomes and sustained corneal permeation	Dai et al. (2013)
Diclofenac	Lipid	Surface-modified liposomes	Increased 1.8-fold concentration in retina–choroid compared to that of the unaltered diclofenac solution	Fujisawa et al. (2012)
Fluconazole	Lipid	Liposomes	Fluconazole-loaded liposomal formulation shown better action as compared to drug solution on Rabbits infected with C. albicans	Habib et al. (2010)
Ciprofloxacin	Lipid	Liposomes	Drug release in controlled manner	Mehanna et al. (2009)
Acetazolamide	Lipid	Liposomes	The positively charged and neutral liposomes exhibited greater lowering in IOP and a more prolonged effect than the negatively charged ones in rabbit eye	Hathout et al. (2007)
Acetazolamide	Lipid	Liposomes	Significant and prolonged decrease in IOP compared to the solution of free drug and plain niosomes	Guinedi et al. (2005)
Atenolol	Lipid	Liposomes	Marked reduction in IOP than solution formulation	Zaid et al. (2003)
ACV	Lipid	Liposomes	Positively charged liposomes increased absorption of ACV, because of a stronger binding effect to the cornea surface than occurs with negatively charged liposomes	Law et al. (2000)
Tropicamide	Lipid	Liposomes	Higher AUC values for tropicamide; this formulation was found to be more effective in dilating the pupil than drug-loaded neutral liposomes	Nagarsenker et al. (1999)
Oligonucleotide	Lipid	Liposomes	Prevent degradation and increase the residence time and efficacy	Bochot et al. (1998)
Acetazolamide	Lipid	Liposomes	Strong and sustained reduction in IOP in rabbits	Omaima et al. (1997)
Pilocarpine	Lipid	Liposomes	Prolonged duration of the miotic effect as compared to aqueous solutions and non-coated vesicles	Durrani et al. (1992)
Penicillin G	Lipid	Liposomes	More than four-fold flux increase across isolated rabbit cornea	Kaur et al. (2004)
Timolol maleate	Non-ionic surfactant	Niosomes	1.7 times higher peak concentration of drug in aqueous humor as compare to the pure timolol maleate solution and 2.34 times AUC higher than TMS	Kaur et al. (2010)
Acetazolamide	Span 60	Niosomes	Permeability increase and increased in aqueous humor drug concentration	Aggarwal et al. (2007)

5-FU, 5-fluorouracil.

Figure 3. Different types of NPs.

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