Ocular Bioavailability Research Articles

Loteprednol-Loaded Nanoformulations for Corneal Delivery by Quality-by-Design Concepts: Optimization, Characterization, and Anti-inflammatory Activity.

Loteprednol etabonate (LE) is a topical corticosteroid that uses inflammatory conditions of the eye. It has a low ocular bioavailability and side effects such as corneal disorder, eye discharge, and ocular discomfort. Therefore, it was decided to select the delivery systems, which are solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nanoemulsion (NE). Design of experiments (DoE) of SLN, NLC, and NE formulations were formulated by using the quality by design (QbD) approach. Precirol® ATO 5 and oleic acid were used as solid and liquid lipids, respectively, in SLN, NLC, and NE formulations. Physiochemical characterization was performed on the formulations. The optimized formulations' inflammatory effects have been appraised on human corneal epithelial cells employing the ELISA test. Physicochemical characterization studies and inflammatory effects were appraised. The sizes of optimized formulations of SLN, NLC, and NE were 86.19nm, 82.38nm, and 126.35nm, respectively, with minimum polydispersity. The release behavior of the formulations is composed of both diffusion and erosion. ELISA test results proved that the formulations significantly reduced IL-1 and IL-6 levels (p < 0.05). D-optimal mixture experimental design allowed us to develop the most precise formulations of SLN, NLC, and NE. Furthermore, the optimized formulations could be promising candidates for treating an inflammation-based corneal disease of the eye.

Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms.

Sufficient ocular bioavailability is often considered a challenge by the researchers, due to the complex structure of the eye and its protective physiological mechanisms. In addition, the low viscosity of the eye drops and the resulting short ocular residence time further contribute to the observed low drug concentration at the target site. Therefore, various drug delivery platforms are being developed to enhance ocular bioavailability, provide controlled and sustained drug release, reduce the number of applications, and maximize therapy outcomes. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) exhibit all these benefits, in addition to being biocompatible, biodegradable, and susceptible to sterilization and scale-up. Furthermore, their successive surface modification contributes to prolonged ocular residence time (by adding cationic compounds), enhanced penetration, and improved performance. The review highlights the salient characteristics of SLNs and NLCs concerning ocular drug delivery, and updates the research progress in this area.

Ocular Nanosuspension a Novel Approach – Review

Effective ocular medication administration is still a difficulty for pharmaceutical scientists in the current drug delivery situation, despite various scientific endeavours. In the ocular drug delivery system, several topical medication applications in the form of solutions, suspensions, and ointments are used to treat eye infections. As a result of several anatomical and pathophysiological barriers present in the eye, many conventional dose forms have issues with poor ocular bioavailability due to short ocular residence times. Many recent available medications have weak solubility, which causes key challenges during formulation and exhibits poor bioavailability. The issue is significantly more complicated for medications that fall under BCS Class II. Nanotechnology is utilised to increase the solubility and bioavailability of poorly soluble medications in order to solve these issues. This review provides an insight into an overview of ocular challenges to anterior section delivery and strategies for removing these obstacles using nanocarrier technology. In addition to addressing the issues of poor solubility and bioavailability, nanosuppension also impacts the pharmacokinetics of the drug, enhancing its efficacy and safety.

Nanostructured Lipid Carriers Aimed to the Ocular Delivery of Mangiferin: In Vitro Evidence

Although mangiferin (MGN) is a natural antioxidant that could be a good candidate for the treatment of ocular diseases, its use in ophthalmology is strongly compromised due to its high lipophilicity. Its encapsulation in nanostructured lipid carriers (NLC) seems to be an interesting strategy for improving its ocular bioavailability. As reported in our previous work, MGN-NLC showed high ocular compatibility and fulfilled the nanotechnological requirements needed for ocular delivery. The aim of the present work was to investigate, in vitro and ex vivo, the capability of MGN-NLC to act as a potential drug delivery system for MGN ocular administration. The data obtained in vitro on arising retinal pigment epithelium cells (ARPE-19) did not show cytotoxic effects for blank NLC and MGN-NLC; likewise, MGN-NLC showed the maintenance of the antioxidant role of MGN by mitigating ROS (Reactive Oxygen Species) formation and GSH (glutathione) depletion induced by H2O2. In addition, the capacity of MGN-released to permeate through and accumulate into the ocular tissues was confirmed ex vivo using bovine corneas. Finally, the NLC suspension has been formulated as a freeze-dried powder using mannitol at a concentration of 3% (w/v) in order to optimize its storage for long periods of time. All this evidence suggests a potential application of MGN-NLC in the treatment of oxidative stress-related ocular diseases.

Design and evaluation of in situ gel eye drops containing nanoparticles of Gemifloxacin Mesylate

Traditional eye drops used for topically administering drugs have poor ocular bioavailability due to the biological barriers of the eye. There is an interest to design and develop novel drug delivery systems that would extend the precorneal residence time, reduce the frequency of administration and decrease dose-related toxicity. This study aimed to prepare Nanoparticles of Gemifloxacin Mesylate and incorporate them into an in situ gel. The nanoparticles were prepared by ionic gelation technique, using 32 factorial design. Sodium tripolyphosphate (STPP) was used to crosslink Chitosan. The optimized formulation of the nanoparticles (GF4) contained 0.15% Gemifloxacin Mesylate, 0.15% Chitosan and 0.20% STPP, producing 71 nm particle size and 81.11% entrapment efficiency. The prepared nanoparticles showed biphasic release, with an initial burst release of 15% in 1.0 hr and a cumulative drug release of 90.53% at the end of 24 hrs. After that, the prepared nanoparticles were incorporated into an in situ gel, using Poloxamer 407, producing a sustained drug release with efficient antimicrobial activity against gram-positive and gram-negative bacteria as confirmed by the cup plate method.

Loteprednol loaded nanoformulations for corneal delivery: Ex-vivo permeation study, ocular safety assessment and stability studies

Loteprednol etabonate (LE) is a topical corticosteroid that is used in inflammatory and allergic conditions of the eye. Nanoformulations including solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nanoemulsion (NE) of LE were prepared for increasing its ocular bioavailability and minimizing the risk of side effects. Nanoformulations were prepared using hot emulsification and ultrasonication technique. The stabilities of the SLN, NLC, and NE were studied at different thermal conditions for 180 days. In this context, alterations in particle size (PS), zeta potential (ZP), viscosity, pH, %EE, and thermal behavior of the formulations were determined. Ex vivo corneal permeation study was performed, subsequently, the tape stripping approach was conducted for defining the LE amount that was blocked by the tear film layer. In addition, to determine the LE amount in epithelial tissue, a homogenization test was performed. the PS of the formulations was between 82.23 and 126.9 nm, and ZPs were between −20.8 mV and −24.6 mV. Furthermore, SLN, NLC, and NE formulations were found to be 2.05, 1.86, and 1.39 times higher LE retained in the cornea against the marketed product, respectively. SLN, NLC, and NE might be alternative delivery systems by reducing the amount of LE for each dose and being used safely based on the results both of MTT and histopathological examinations as well.

Improving ocular bioavailability of hydrophilic drugs through dynamic covalent complexation.

The clinical benefits of diquafosol tetrasodium (DQS), a hydrophilic P2Y2 receptor agonist for dry eye, have been hindered by a demanding dosing regimen. Nevertheless, it is challenging to achieve sustained release of DQS with conventional drug delivery vehicles which are mainly designed for hydrophobic small molecule drugs. To address this, we developed an affinity hydrogel for DQS by taking advantage of borate-mediated dynamic covalent complexation between DQS and hydroxypropyl guar. The resultant formulation (3% DQS Gel) was characterized by sustained release, low corneal permeation, and extended ocular retention, which were desirable attributes for ocular surface drug delivery. Both in vitro and in vivo studies had been carried out to verify the biocompatibility of 3% DQS Gel. Using corneal fluorescein staining, the Schirmer's test, PAS staining, quantitative PCR and immunohistological analyses as outcome measures, the superior therapeutic effects of 3% DQS Gel over PBS, the hydrogel vehicle and free DQS were demonstrated in a mouse dry eye model. Our DQS delivery strategy reported herein is readily applicable to other hydrophilic small molecule drugs with cis-diol moieties, thus providing a general solution to improve clinical outcomes of numerous diseases.

Recent Progress in Chitosan-Based Nanomedicine for Its Ocular Application in Glaucoma.

Glaucoma is a degenerative, chronic ocular disease that causes irreversible vision loss. The major symptom of glaucoma is high intraocular pressure, which happens when the flow of aqueous humor between the front and back of the eye is blocked. Glaucoma therapy is challenging because of the low bioavailability of drugs from conventional ocular drug delivery systems such as eye drops, ointments, and gels. The low bioavailability of antiglaucoma agents could be due to the precorneal and corneal barriers as well as the low biopharmaceutical attributes of the drugs. These limitations can be overcome by employing nanoparticulate drug delivery systems. Over the last decade, there has been a lot of interest in chitosan-based nanoparticulate systems to overcome the limitations (such as poor residence time, low corneal permeability, etc.) associated with conventional ocular pharmaceutical products. Therefore, the main aim of the present manuscript is to review the recent research work involving the chitosan-based nanoparticulate system to treat glaucoma. It discusses the significance of the chitosan-based nanoparticulate system, which provides mucoadhesion to improve the residence time of drugs and their ocular bioavailability. Furthermore, different types of chitosan-based nanoparticulate systems are also discussed, namely nanoparticles of chitosan core only, nanoparticles coated with chitosan, and hybrid nanoparticles of chitosan. The manuscript also provides a critical analysis of contemporary research related to the impact of this chitosan-based nanomedicine on the corneal permeability, ocular bioavailability, and therapeutic performance of loaded antiglaucoma agents.

Ophthalmic Drug Delivery: New Dimensions

The objective of this review is to compile updated scientific information on the conventional and novel approaches to the ocular delivery of medication. Owing to the special features and requirements of a specific site delivery system, there is a need for the refinement of novel drug delivery systems. The conventional ocular dosage forms often possess problems like quick pre-corneal drug excretion because of its nasolacrimal drainage which may lead to tearing turnover and finally result in low ocular bioavailability. The design of novel delivery systems helps in delivering the therapeutic agent very efficiently into the desired areas of the eyes by their unique particle size and also because of their biocompatibility with ocular tissues. In addition, they also offer good contact time, improved drug loading, and releasing properties with less drug loss and low toxicity. All these advantages of a novel delivery system directly cause an improvement in the patient’s satisfaction and the bioavailability of the therapeutic agent. In this review article, information about the different ocular novel drug delivery systems such as nanoparticles, liposomes, niosomes, microneedles, and dendrimers is summarized and discussed. Noteworthy contributions by various researchers in the field of these delivery systems have been also been mentioned. Therefore, this article will be beneficial for future researchers and formulation developers working on the design and development of ocular therapeutic delivery systems.

Proniosomes: A pro vesicular system in ocular drug delivery

The eyes are the only sense organ required for vision. Diseases like glaucoma, cataract, diabetic retinopathy etc. affect the proper functioning of the eyes and sometimes lead to blindness. The treatment of eye disorders is very challenging because of the unique structure of this organ. The traditional treatment approaches are not effective in providing good ocular bioavailability. The Provesicular systems are new-generation delivery systems that can improve drug bioavailability and provide therapeutic responses in a controlled manner for desired time. Among all, liposomes are the first such delivery vehicle but due to the lack of stability and the high cost, niosomes were formulated. Niosomes are nanosized vesicles composed of non-ionic surfactants that can encapsulate both lipophilic and hydrophilic drugs. The drawbacks associated with niosomes, like fusion, aggregation, sedimentation, difficulty in sterilization, leaking, etc., gave birth to proniosomes. Proniosomes are more stable and bioavailable than niosomes and liposomes. Proniosomes are dry formulations of hydrophilic carrier particles coated with a water-soluble non-ionic surfactant that, when hydrated, instantly transforms into niosomes. Proniosomes can be used as stable, non-toxic carriers to improve the ocular residence and bioavailability of many drugs. This paper reviewed various aspects of proniosomes along with their biomedical applications and toxicity in ocular drug delivery.

Antifungal Combination Eye Drops for Fungal Keratitis Treatment.

Fungal keratitis (FK) is a corneal mycotic infection that can lead to vision loss. Furthermore, the severity of FK is aggravated by the emergence of resistant fungal species. There is currently only one FDA-approved formulation for FK treatment forcing hospital pharmacy departments to reformulate intravenous drug preparations with unknown ocular bioavailability and toxicity. In the present study, natamycin/voriconazole formulations were developed and characterized to improve natamycin solubility, permanence, and safety. The solubility of natamycin was studied in the presence of two cyclodextrins: HPβCD and HPγCD. The HPβCD was chosen based on the solubility results. Natamycin/cyclodextrin (HPβCD) inclusion complexes characterization and a competition study between natamycin and voriconazole were conducted by NMR (Nuclear Magnetic Resonance). Based on these results, several eye drops with different polymer compositions were developed and subsequently characterized. Permeability studies suggested that the formulations improved the passage of natamycin through the cornea compared to the commercial formulation Natacyn®. The ocular safety of the formulations was determined by BCOP and HET-CAM. The antifungal activity assay demonstrated the ability of our formulations to inhibit the in vitro growth of different fungal species. All these results concluded that the formulations developed in the present study could significantly improve the treatment of FK.

Development of Besifloxacin HCL Loaded Ocular İn Situ Gels; In Vitro Characterization Study

Objective: The aim of this study is to develop in situ gel formulations containing besifloxacin hydrochloride are heat triggered, which are prepared by using different poloxomer and derivatives different polymers that will change the gelling temperature to increase corneal contact time, regulate drug release, improve ocular bioavailability and increase patient compliance increase mucoadhesion.&#x0D; Material and Method: Various concentrations of poloxamer 188 (P188) and poloxamer 407 (P407) were used to create the in situ forming gels. To increase the gel's capacity for bioadhesion, mucoadhesives such hydroxypropylmethyl cellulose (HPMC) or hydroxyethyl cellulose (HEC) were included in the formulations. Drug release in vitro, sol-gel transition temperature, rheological behavior, pH, clarity, and mucoadhesion force were all assessed for the produced formulations. &#x0D; Result and Discussion: The developed formulations' gelation temperatures ranged from 29 to 35°C. The preparations' viscosity and mucoadhesion force increased with increasing P407, HPMC, and HEC concentrations. Besifloxacin HCl forms in situ gel formulas with K1, K2, K3, and K6 suited for mucoadhesion characteristics, gelation temperature, and viscosity. These formulations exhibit pseudoplastic flow. Increasing polymer concentrations resulted in a reduction in the burst release of the formulations. However, at the end of 6 hours, drug release was finished in all formulations. The results show that in situ gels containing P407 and P188 show promise for besifloxacin HCl application

Nanogel Development and its Importance in Ophthalmic Drug Delivery System

Background: The current review focuses on ophthalmic nanogels, their applications, their benefits over traditional gels, and the challenges and opportunities of nanogels. The major goal is to investigate ophthalmic nanogels from preparation through characterization and how nanogels are the future of the ophthalmic drug delivery system compared to traditional gels, eye drops, and ointments. Objective: Because of the ophthalmic bioavailability, delivery to the eye is crucial. The lacrimal flu-id in the eye clears the eye surface, and the ocular sight is washed away as a result of this medicine. The limited ocular bioavailability was also due to the different obstacles present. Drug nano-gelling systems are effective in improving ocular bioavailability and corneal permeation time. Nanoparti-cles abound in these nanogels. Various natural polymers, such as Chitosan and Alginate, and syn-thetic polymers, such as PLA and PLGA, can be used to make nanogels. The use of nanotechnology improves medicine bioavailability and penetration in the eye. However, nanotechnology has some limits, such as large-scale manufacturing, restricting medicine doses, and so forth. Conclusion: Nanotechnology offers much clinical potential when it comes to treating eye issues. Although ophthalmic nanogels are suited for effective drug delivery, they must meet several re-quirements. First, the drug component must be encapsulated adequately in a stable polymer com-plex. In ocular drug delivery, nanogels are a preferable option since they can improve patient com-pliance and therapeutic impact. In addition, the nanogel has a faster corneal penetration time and higher bioavailability.

Long-acting acid-sensitive ketal-linked dexamethasone microcrystals for treating experimental autoimmune uveitis.

Corticosteroids have for some time been used as first-line drugs for the topical treatment of noninfectious uveitis, but poor ocular bioavailability and the rapid clearance of eye drops necessitate frequent dosing, reducing patient compliance. In this study, we used an acid-sensitive stearoxyl-ketal-dexamethasone pro-drug microcrystals (SKD MCs), which is consistently safe and effective in the control of uveitis inflammation in rats. We used a rat model of experimental autoimmune uveitis (EAU) to evaluate the effects of SKD MCs in terms of clinical manifestations, molecular biology, pathological histology, and visual electrophysiology compared to dexamethasone sodium phosphate injection or phosphate-buffered saline. SKD MCs significantly reduced inflammation in EAU, improved the ability to suppress inflammatory cytokines and to protect retinal function, and significantly reduced retinal microglia activation, with no increase in intraocular pressure throughout the treatment. Our results indicate that the SKD MCs formulation holds promise as a new strategy for the treatment of noninfectious uveitis and potentially other ocular inflammatory diseases.

Chitosan/HPMC-based mucoadhesive film co-loaded with fluconazole and ofloxacin for management of polymicrobial keratitis

Bacterial and fungal co-infection leads to polymicrobial keratitis (PMK). The current study produced swellable mucoadhesive biopolymeric films composed of chitosan, HPMC, and glycerol using cast drying method. The film was dual-loaded with fluconazole (FCZ) and ofloxacin (OFX) to treat PMK. The prepared film exhibited excellent thickness, folding endurance, surface pH, tensile strength, and stability characteristics. In addition, it also exhibited good in vitro antimicrobial activity, ex-vivo mucoadhesion, and corneal permeation. AUC (0-∞) and MRT were 6.5 and 5.2-fold higher for a film containing FCZ and 22.5 and 2.5-fold higher for a film containing OFX than their marketed formulations. PK-PD simulation study supports desired efficacy of the proposed dosage form. Thus, the film exhibits longer pre-corneal drug residence time and enhanced ocular bioavailability, most likely resulting in high patient compliance. The proposed film could be a prominent replacement for the existing dosage form and may present a viable alternative for the treatment of PMK.

Aqueous Prostaglandin Eye Drop Formulations.

Glaucoma is one of the leading causes of irreversible blindness worldwide. It is characterized by progressive optic neuropathy in association with damage to the optic nerve head and, subsequently, visual loss if it is left untreated. Among the drug classes used for the long-term treatment of open-angle glaucoma, prostaglandin analogues (PGAs) are the first-line treatment and are available as marketed eye drop formulations for intraocular pressure (IOP) reduction by increasing the trabecular and uveoscleral outflow. PGAs have low aqueous solubility and are very unstable (i.e., hydrolysis) in aqueous solutions, which may hamper their ocular bioavailability and decrease their chemical stability. Additionally, treatment with PGA in conventional eye drops is associated with adverse effects, such as conjunctival hyperemia and trichiasis. It has been a very challenging for formulation scientists to develop stable aqueous eye drop formulations that increase the PGAs’ solubility and enhance their therapeutic efficacy while simultaneously lowering their ocular side effects. Here the physiochemical properties and chemical stabilities of the commercially available PGAs are reviewed, and the compositions of their eye drop formulations are discussed. Furthermore, the novel PGA formulations for glaucoma treatment are reviewed.

PREPARATION AND EVALUATION OF TMC LOADED VORICONAZOLE NANOPARTICLES

Objective: Ocular diseases affect a growing number of people across the globe. Hence, the present research work focused to prepare and evaluate voriconazole (VCZ) nanoparticles containing trimethyl chitosan (TMC) for ophthalmic drug delivery with primary goal is to develop topical ocular delivery systems with improved ocular bioavailability and reduced systemic side effects while maintaining the dosage form’s simplicity and convenience. Methods: In the present study, the nanoparticles are prepared using ionotropic gelation method. The physiochemical interactions between drugs and selected excipients were studied using various techniques such as FTIR, DSC, XRD, and H-NMR. The physiochemical properties of the nanoparticles such as size, PDI, pH, and drug content/entrapment efficiency were determined. The in-vitro drug release properties were characteristics and examined for the formulations. The synthesize form of chitosan, that is, tri-methyl chitosan is used due to solubility issue. Result: The comparative study was done using TMC and cyclodextrin as a polymer out of which TMC polymer gives better results. The optimization is done using 32 factorial design using design expert software. The optimized batch follows the zero order release kinetics. Conclusion: TMC loaded VCZ nanoparticles show better result with improved solubility and permeability.

Formulation and Evaluation of Ophthalmic Novel In-Situ Gel Containing Acyclovir for the Treatment of Herpes Simplex Keratitis

Herpes Simplex Keratitis (HSK), which is a major reason of corneal infection. The virus (Herpes simplex virus) enters into a latent phase. It presents primary infection as conjunctiva and eyelids swelling and mild inflammation. According to global research of disease, it is around 1.4 million, including 38,000 new cases of visual impairment or blindness every year. Several oral and topical antiviral drugs for HSK are out there commercially. However, toxicity and low patient compliance hamper use in HSK. Thus, an effective and safe delivery for HSK is required. The conventional ocular delivery systems such as suspension, solutions and ointments show drawbacks like increased low efficiency, pre-corneal elimination and blurred vision respectively, resulting to poor bioavailability. Ophthalmic In-situ gels, which are viscous polymer-based liquids are instilled in eyes as drops that undergoes sol-to-gel transition that improve duration of corneal contact and ocular bioavailability and thereby reducing frequency of administration. Merits of Ophthalmic in-situ gels over conventional dosage forms are possibility of releasing drugs at constant and slow rate with increased ocular residence time, increased shelf life and accurate dosing. This research includes ion induced in-situ-forming polymeric systems using combination of gelling agents to prolong corneal contact time, eradicate drug elimination and increase the bioavailability.

Oil-free eye drops containing Cyclosporine A/cyclodextrin/PVA supramolecular complex as a treatment modality for dry eye disease

According to the global mapping of dry eye disease (DED), nearly 5 to 50 % of people suffer from DED, and this number is on the rise. The drug of choice Cyclosporine A (CsA) exhibits poor ocular bioavailability due to high molecular weight and lipophilicity. Moreover, formulations of CsA currently available are in the form of oil-based emulsions that are known to cause ocular irritation and pain. In this study, sulfobutylether-β-cyclodextrin (SBE-β-CD) based binary and ternary supramolecular complexes of CsA were developed as completely oil-free, and particle-free eye drops to treat DED. The physicochemical characterizations were supplemented with relevant in silico studies, to ascertain the findings. Further, the efficacy of the complexes was evaluated in the scopolamine-induced mouse model of DED. The complexation improved the CsA solubility by ~21-fold, with ~4-fold improvement in dissolution and transcorneal permeation. The non-irritancy and non-toxicity were confirmed by hen's egg chorioallantoic membrane assay and cytotoxicity assay using human corneal epithelial cells, respectively. The in vivo treatment with the ternary CD complex demonstrated better management of the dry eye supported by the tear volume assessment, corneal fluorescein staining, and histopathological studies of the cornea, lacrimal gland, and harderian gland. The study demonstrates the potential of the supramolecular complex as an alternative to the oil-based formulation of eye drops for drugs that show low solubility and poor corneal permeation.

Linoleic Acid-Based Transferosomes for Topical Ocular Delivery of Cyclosporine A.

Delivering high-molecular-weight hydrophobic peptides, such as cyclosporine A, across the corneal epithelium remains a challenge that is complicated by other physio-anatomical ocular structures that limit the ocular bioavailability of such peptides. Transferosomes have previously been used to improve transdermal permeability, and have the potential for improving the ocular corneal permeability of applicable drugs. In this study, transferosomes for the potential ocular delivery of cyclosporine A were investigated. Linoleic acid was evaluated for its effect on the stability of the transferosomes and was substituted for a portion of the cholesterol in the vesicles. Additionally, Span® 80 and Tween® 80 were evaluated for their effect on transferosome flexibility and toxicity to ocular cells as edge activators. Attenuated Total Reflectance–Fourier Transform Infrared spectroscopy (ATF-FTIR), differential scanning calorimetry (DSC), and dynamic light scattering (DLS) were used to evaluate the physicochemical parameters of the blank and the cyclosporine A-loaded transferosomes. Cyclosporine A release and corneal permeability were studied in vitro and in a New Zealand albino rabbit corneal model, respectively. The linoleic acid contributed to improved stability and the nano-size of the transferosomes. The Tween®-based formulation was preferred on the basis of a more favorable toxicity profile, as the difference in their corneal permeability was not significant. There was an initial burst release of cyclosporine A in the first 24 h that plateaued over one week. The Tween®-based formulation had a flux of 0.78 µg/cm2/h. The prepared transferosomes demonstrated biocompatibility in the ocular cell line, adequately encapsulated cyclosporine A, ensured the corneal permeability of the enclosed drug, and were stable over the period of investigation of 4 months at −20 °C.