Cortical spreading depression (SD) is the likely cause of migraine aura and a putative headache trigger. Migraine treatments, including triptans and calcitonin gene related peptide (CGRP) receptor antagonists, are limited by poor bioavailability. This study evaluates whether intranasally administered poly lactic co-glycolic acid (PLGA) based hybrid nanoparticles (HNPs) encapsulating rizatriptan (RZT) could provide sustained drug release, enhance brain delivery, and improve therapeutic efficacy against periorbital allodynia triggered by optogenetic SD in mice. CGRP8-37 was conjugated to the nanoparticle surface (HNP-CGRP8-37) and RZT encapsulated whitin HNPs (HNP-RZT). were intranasally administered alone or in combination and compared with intraperitoneal CGRP8-37 and RZT. Formulations were characterized for particle size, zeta potential, and polydispersity index, and assessed for in vitro drug release, cytotoxicity, and in vivo brain RZT concentrations. In the acute SD model, periorbital allodynia was evaluated 1 h after a single SD. In the repeated SD paradigm, seven SDs were induced every other day, and periorbital thresholds were assessed up to 6 days after the final SD. HNPs exhibited uniform particle size (<200 nm), positive zeta potential, and low polydispersity. RZT release from HNP-RZT was sustained in vitro. Intranasal HNP-RZT demonstrated prolonged brain RZT retention compared with intraperitoneal RZT. In the acute SD model, HNP-RZT did not reach statistical significance (p = 0.065), whereas intraperitoneal RZT significantly increased periorbital thresholds. In contrast, in the repeated SD model, HNP-RZT demonstrated delayed but persistent suppression of allodynia compared with intraperitoneal RZT. These findings support the potential of intranasal nanoparticle-based delivery to prolong central exposure of RZT and enhance therapeutic durability in chronic SD conditions.

Hydrogels are three-dimensional, crosslinked polymeric systems with high hydrophilicity and biocompatibility, making them ideal materials for wound healing applications. In this study, a silver nanoparticle (AgNP)-loaded chitosan–poly (vinyl alcohol) (CS–PVA) hydrogel was developed using a novel, simple, and cost-effective approach. In this approach, sodium borohydride (NaBH₄) simultaneously acts as a reducing agent for AgNP synthesis and as a physical crosslinking agent for hydrogel formation. AgNPs were synthesized via NaBH₄-mediated reduction and characterized by dynamic light scattering and UV–Vis spectroscopy. The resulting hydrogels were evaluated by Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), scanning electron microscopy (SEM), Energy-dispersive X-ray (EDS) spectroscopy, swelling, porosity and mechanical test. In vitro biocompatibility and wound healing potential were assessed using cell viability assays and a scratch wound assay. Among all formulations, M30, an AgNP-loaded CS–PVA hydrogel, prepared with medium molecular weight (MMW) chitosan and 30 mL of AgNP suspension, had the best overall performance with the highest swelling degree, favorable mechanical performance. It maintained cell viability above 80

Chemotherapy-induced nausea and vomiting (CINV) typically occurs in two distinct phases: an acute phase, which arises within the first 24 h following chemotherapy, and a delayed phase, which develops between 24 and 120 h afterward. While acute CINV is now effectively controlled using 5-hydroxytryptamine type 3 (5-HT3) receptor antagonists, managing delayed CINV remains a significant clinical challenge. This study was aimed to develop Ondansetron hydrochloride (OND), loaded nanocarriers featuring high encapsulation efficiency (EE), to enable sustained drug release over several days. OND loaded sustained release liposome and lipid polymer hybrid polymeric nanoparticle (LPHNP) were prepared. The prepared formulations were characterized in terms of particle size and distribution, zeta potential, encapsulation efficiency and drug release in an in vitro study. The effects of the type of phospholipids, phospholipid/cholesterol molar ratio, and pH of hydration medium on liposome formulations were examined. In LPHNP formulations, the effect of external water phase volume, phospholipid type, preparation method, and pH of the aqueous phase was evaluated. In vitro cytotoxicity of the formulations was determined using L929 fibroblast cells. Optimum LPHNP formulation and the commercial product (Zofer (R)) were administered subcutaneously in a single dose to Wistar albino rats. It was found higher Cmax and MRT in LPHNP formulations than Zofer (R). In this study, the effectiveness and safety of Ondansetron hydrochloride loaded LPHNP formulations were determined.

Magnetic Resonance Imaging (MRI) is a crucial diagnostic modality in modern medical practice, offering non-invasive insight into internal structures and functions of the human body. The development of MRI contrast agents has significantly improved imaging sensitivity and precision. Traditional gadolinium-based agents, while effective, have been linked to nephrogenic systemic fibrosis (NSF), necessitating the exploration of alternative contrast agents. Nanoparticle-based systems have emerged as promising candidates for new contrast media, leveraging the unique properties of nanoparticles to address technological and medical challenges. Manganese has garnered attention due to its potential as a safe and effective alternative to gadolinium-based agents. This study delves into the synthesis of manganese loaded nanoparticles using poly (lactic-co-glycolic acid) (PLGA), a biodegradable polymer with proven biocompatibility. Two distinct manganese nanoencapsulation methods were devised and evaluated for their toxicity profiles. The method demonstrating superior biocompatibility, designated as PLGA-MN, was selected for in vivo assessments. Comparative analysis was performed against a control group administered manganese acetate (MnAc) (PBS) solution. In vivo MR imaging was performed on Sprague-Dawley rats, while the distribution of PLGA-MNs in blood, brain, liver, and spleen was determined through inductively coupled plasma mass spectrometry (ICP-MS). The results lay the foundation for advancing contrast agent development, harnessing nanotechnology to elevate diagnostic imaging capabilities and simultaneously addressing the safety considerations linked to conventional agents such as gadolinium.

Keratoconus is a progressive disease characterized by corneal thinning and conical deformation. Corneal cross-linking, a common treatment, strengthens collagen fibers using vitamin B2 (riboflavin) and UVA light. However, the surgical removal of the corneal epithelium (Epi-Off) required for riboflavin penetration causes complications and may affect treatment success. To address this, research has focused on delivering riboflavin without removing the epithelium (Epi-On). In this study, riboflavin-based hydrogel and co-crystal formulations were developed and evaluated through in vitro, ex vivo, and in vivo studies. Co-crystals were prepared using trehalose, dextrose, mannitol, and nicotinamide as agents, employing solvent evaporation and co-mixing methods. These formulations were characterized using DSC (Differential Scanning Calorimetry), XRD (X-Ray Diffraction), and FTIR (Fourier Transform Infrared Spectroscopy), identifying 1R1N (1 unit mol riboflavin and 1 unit mol nicotinamide co-crystals) and 1R1M (1 unit mol riboflavin and 1 unit mol mannitol co-crystals) groups as promising candidates. Thermosensitive hydrophilic gels containing riboflavin or riboflavin-5-phosphate sodium and Transcutol P (a permeation enhancer) were also developed, using Pluronic F-127 as the polymer. The 18 % Pluronic F-127 gel formed at 31.4 ± 0.2 °C. Drug release studies showed faster release from riboflavin-5-phosphate sodium formulations, while ex vivo retention studies revealed higher corneal retention for co-crystals. In vivo studies on rat corneas demonstrated superior drug concentrations for riboflavin formulations compared to riboflavin-5-phosphate sodium, with hydrophilic gels showing prolonged corneal contact time. The THJ-TP formulation (Riboflavin-5-phosphate sodium and permeation enhancer (Transcutol P) containing hydrophilic gel formulations), containing riboflavin-5-phosphate sodium and Transcutol P, emerged as the most promising candidate. This research represents a significant advancement towards a non-invasive riboflavin-based treatment for keratoconus.

Cystic echinococcosis is the metacestode stage of Echinococcus granulosus and is a worldwide public health problem. Today, various difficulties in the treatment of cystic echinococcosis limit the treatment of cystic echinococcosis. In this study, the in vitro activity of PLGA nanoparticles loaded with albendazole sulfoxide and praziquantel and targeted with phytase enzyme on Echinococcus granulosus micro-hydatid cysts was evaluated as a new formulation. For this purpose, first conjugation of PLGA polymer and phytase enzyme was performed, then albendazole sulfoxide and praziquantel loaded nanoparticles were prepared using PLGA-phytase polymer and characterization studies were performed. Permeability and cytotoxicity tests were carried out with cell culture studies of the formulations for which characterization studies were performed and it was found that the formulations did not show any cytotoxic effect. In order to evaluate the formulations, micro-hydatid cysts were developed in vitro with Echinococcus granulosus protoscoleces collected from slaughterhouse animals and the formulations were applied. In vitro hydatid cyst viability studies, approximately 50 % of cysts died on day 4 in the group applied with the combination of 10 mu g/mL free albendazole sulfoxide and 50 mu g/mL free praziquantel, while 100% of cysts died in the group applied with the new formulation containing the same amount of drug. In addition, ex vivo studies on the laminar layer of hydatid cysts obtained from sheep liver showed that the new formulation binds to the laminar layer and increases the permeability of albendazole sulfoxide and praziquantel across the laminar layer by approximately 2-fold.

The skin, which is a protective barrier for the human body, can be injured from time to time as a result of disease or trauma. Electrospun nanofiber wound dressings made from biopolymers for skin regeneration and wound healing have been widely investigated in recent years. This study successfully prepared PVA-based nanofiber wound dressings loaded with nicotine and quercetin by the electrospinning method to accelerate wound healing. The nanofibers were characterized morphologically, physically, and chemically, and then their cytotoxicity levels and effects on wound healing were evaluated in vitro. First, three different concentrations of PVA solutions were prepared, and one nanofiber wound dressing was produced with each of them. Next, characterization studies of the nanofiber wound dressings were performed, and the optimal formulation was selected. Morphological examinations by SEM analysis revealed that homogeneous and uniform nanofibers with an average diameter of 122.11 ± 36.22 nm and no bead formation were successfully produced. The structural properties of the nanofiber wound dressings were evaluated by DSC and FTIR analyses, which revealed that there was no significant physico-chemical interaction between the polymer and the loaded drugs. In terms of drug loading efficiency, the loading efficiency of nicotine was found to be higher compared to quercetin (quercetin: 21.86 ± 2.1

Albendazole sulfoxide (ALBSOX) and Praziquantel (PRZ) are broad-spectrum anthelmintic medications used in the treatment of both humans and animals that are challenging to manufacture for geriatric and pediatric populations and have poor oral bioavailability due to their low water solubility and high lipophilicity. To increase the solubility and bioavailability of the drugs, ALBSOX and PRZ-loaded nanofiber films were prepared using polyvinylpyrrolidone K90 (PVP), a non-toxic, inert polymer with high hydrophilic characteristics. SEM analysis of the produced ALBSOX and PRZ-loaded PVP nanofiber films revealed them to be uniform and smooth, with good uniformity and mechanical properties. The PVP nanofiber films of ALBSOX and PRZ disintegrated in phosphate buffer (pH 6.8) in less than 1 s and increased the solubility of ALBSOX and PRZ about five times compared to pure active ingredients. Furthermore, the prepared ALBSOX and PRZ-loaded PVP nanofiber films were found to have no cytotoxic effect in cell viability studies using L929 cells, and increased the protoscolicidal effect of the ALBSOX and PRZ combination approximately 2-fold in studies of Echinococcus granulosus protoscoleces. The findings of the present study reveal that the developed PVP nanofiber films have the potential to improve the dissolution profile and pharmacological efficacy of the ALBSOX and PRZ.

M3, a condensed 1,4-dihydropyridine (DHP) derivative, targets both L- and T-type calcium channels and therefore, stands as a promising antihypertensive drug candidate. This study aims to improve the poor solubility of M3 using nanocrystal technology (a combination of precipitation and ultrasonication methods) to enhance its oral bioavailability. Pre-formulation studies were performed and M3 nanosuspensions were prepared using different stabilizers (polyvinyl pyrrolidone K30, polyvinyl alcohol, SoluPlus & REG;) and surfactants (poloxamer 188, poloxamer 407, sodium deoxycholate, sodium lauryl sulfate) at different concentrations (0.05, 0.1, 0.5, 1.0, 2.0%, w/v). The optimum nanosuspension formulation was freeze-dried using different cryoprotectants (mannitol, trehalose, glucose, sucrose, dextran) at different ratios (1.25, 2.5, 5.0%, w/v). It was determined that the most suitable cryoprotectant and ratio was 5.0% trehalose, resulting in nanocrystals with a size of 320.2 & PLUSMN; 15.3 nm and a zeta potential of -27.4 & PLUSMN; 0.1 mV. The physicochemical properties of M3, poloxamer 188, physical mixture and freeze-dried nanocrystals were evaluated by XRD, DSC and FT-IR analyses. Characterization studies showed amorphization of M3 in the freeze-dried nanocrystals prepared with poloxamer 188. The result of equilibrium solubility and permeability studies results indicated that M3 could be a BCS class 4 compound. Cell culture studies using Caco-2 cells showed that M3 had no significant toxic effect on the cells and had a Papp value of 2.2 x 10-7 cm/s. Compared to coarse M3 powder freeze-dried M3 nanocrystals showed a 200-fold increase in solubility and a 28.6-fold increase in apparent permeability. The cytotoxic effect of M3 was also reduced by using poloxamers as stabilizers in the formulation. M3 nanosuspensions were found to be a promising candidate for the oral administration of M3 for the potential treatment of hypertension due to the increase in solubility and permeability which could enhance its oral bioavailability.

Prostate cancer is a global disease that negatively affects the quality of life. Although various strategies against prostate cancer have been developed, only a few achieved tumor-specific targeting. Therefore, a special emphasis has been placed on the treatment of cancer using nano-carrier-encapsulated chemotherapeutic agents conjugated with tumor-homing peptides. The targeting strategy coupling the drugs with nanotechnology helps to overcome the most common barriers, such as high toxicity and side effects. Prostate-specific membrane antigen has emerged as a promising target molecule for prostate cancer and shown to be targeted with high affinity by GRFLTGGTGRLLRIS peptide known as peptide 563 (P563). Here, we aimed to assess the in vitro and in vivo targeting efficiency, safety, and efficacy of P563-conjugated, docetaxel (DTX)-loaded polymeric micelle nanoparticles (P563-PEtOx-co-PEI30%-b-PCL-DTX) against prostate cancer. To this end, we analyzed the cytotoxic activity of P563-PEtOx-co-PEI30%-b-PCL and P563-PEtOx-co-PEI30%-b-PCL-DTX by a cell proliferation assay using PNT1A and 22Rv1 cells. We have also determined the targeting selectivity of P563-PEtOx-co-PEI30%-b-PCL-FITC by flow cytometry and assessed the induction of cell death by western blot and TUNEL assays for P563-PEtOx-co-PEI30%-b-PCL-DTX in 22Rv1 cells. To investigate the in vivo efficacy, we administered DTX in the free form or in polymeric micelle nanoparticles to athymic CD-1 nu/nu mice 22Rv1 xenograft models and performed histopathological analyses. Our study showed that targeting prostate cancer with P563-conjugated PEtOx-co-PEI30%-b-PCL polymeric micelles could exert a potent anti-cancer activity with low side effects.

Low molecular weight heparins (LMWHs) are only used parenterally. They have low oral absorption and bioavailability due to their high anionic charge density, exposure to enzymatic degradation and first-pass effect. The aim of this study was the development and evaluation of nanodelivery systems to increase the oral bioavailability of enoxaparin (low molecular weight heparin). In line with this goal, three nanosystems, such as three-layered nanofiber membrane (NF), enoxaparin loaded nanoparticles (NP) and three-layered nanofiber membrane loaded with enoxaparin nanoparticles (NP/NF) were prepared. As a result of the SEM images of nanofiber membranes, the surfaces of the fibers were found to be smooth and the fiber diameters were between 300 and 500 nm. Enoxaparin amount was found to be 390-400 mu g/cm2 for nanofiber membranes. Porosity, specific surface area, contact angle, and work of mucoadhesion values were found to be 53.78%, 9.46 m2/g, 113.39 degrees, 0.19 mJ/cm2 for NF formulation and 50.52%, 3.04 m2/g, 104.96 degrees, 2.65 mJ/cm2 for NP/NF formula-tion, respectively. In vitro dissolution studies showed that less than 20% of the drug was released from the nanofibers at the end of 2 h in acidic pH. MTT studies showed that cell viability was more than 80%. Stability studies showed that there was no significant changes at three different storage conditions. In conclusion, nanodelivery systems were successfully prepared to increase the oral bioavailability of enoxaparin and to protect it from the acid pH of the stomach.

A simple, rapid and reproducible HPLC method has been developed and validated for the quantification of albendazole sulfoxide (ALBSOX) and praziquantel (PRZ), which can coexist in various dosage forms. Chromatographic separation was performed in gradient mode using a mobile phase consisting of an InertSustain (R) C18 column (150 x 4.6 mm, 5 mu m) and acetonitrile: water (v/v) at a flow rate of 1.0 mL/min. The active substance peaks were well separated and detected by a DAD detector at 217 nm. The HPLC method was linear for ALBSOX and PRZ in the concentration range of 0.1-50 mu g/mL. Limit of detection (LOD) was found to be 0.01 mu g/mL for ALBSOX and 0.009 mu g/mL for PRZ. The limit of quantification (LOQ) was found to be 0.03 mu g/mL for ALBSOX and 0.027 mu g/mL for PRZ. The developed HPLC method was validated based on ICH guidelines for specificity, linearity, system suitability, precision and accuracy. The method was applied for simultaneous quantification and characterization studies of ALBSOX and PRA in PLGA nanoparticles.

Objectives:Daidzein (DZ), a water-insoluble isoflavone, has many beneficial effects (anti-inflammatory, antioxidant, and anticancer effects, etc.) on human health. DZ has a very low oral bioavailability related to its physicochemical properties (low solubility, intense metabolism of DZ in the intestine and liver). This study aimed to prepare and in vitro characterize the nanosuspension formulations of DZ to improve the poor solubility and efficacy of DZ.Materials and Methods:DZ nanosuspension formulations were prepared with media milling technique using zirconium oxide beads as milling media. Pluronic F127 and polyvinylpyrrolidone (PVP) K30 (formulation A; F-A) and sodium dodecyl sulfate (SDS) (SDS + pluronic F127 + PVP K30; formulation B; F-B) were used as stabilizers. The nanosuspension formulations were evaluated for morphological properties, particle sizes, zeta potential, DZ content, saturation solubility, dissolution, and their cytotoxic effects on RG2 glioblastoma tumor cells.Results:F-A and F-B formulations were nanosized (in the range of about 181-235 nm) and had negative zeta potential values before and after lyophilization. The DZ content of F-A and F-B formulations were found to be 93.68±0.78% and 89.75±0.49%, respectively. Fourier transform infrared spectroscopy analysis showed that there was no significant interaction between DZ and the excipients. Differential scanning calorimetry and X-ray diffraction analyses confirmed no change in the crystal structure of DZ in F-A and F-B formulations.Conclusion:In this study, the nanosuspension formulations were successfully prepared and characterized in vitro. Nanosuspension formulations increased the saturation solubility, dissolution rate, and cytotoxic effect of DZ.

The encapsulation of hydrophilic drugs is still a challenge due to their tendency to leak into the outer aqueous phase. The aim of the study is to develop and evaluate Ondansetron HCl (OND) loaded controlled release polymeric nanoparticles with high encapsulation efficiency (EE). Polymeric nanoparticles (PNPs) were prepared with two different types of polycaprolactone and five different types of poly (d, l-lactide-co-glycolide) (PLGA) by the double emulsion solvent evaporation method. The effects of formulation variables on the particle size, zeta potential, encapsulation efficiency, and drug release of OND loaded PNPs were investigated. The particle size, PDI, and zeta potential of the optimum formulation were 342.5 +/- 6.7 nm, 0.240 +/- 0.020, and 20.1 +/- 0.51 mV, respectively, whereas the encapsulation efficiency was 46.8 +/- 2.78%. The optimum formulation was pegylated to prolong the residence time in circulation. Transmission electron microscopy (TEM) images confirmed the spherical shape of nanoparticles. Pegylated formulation had 47.76 +/- 1.69% encapsulation efficiency and sustained release profile (92.7 +/- 5.7% in 72 h). Differential Calorimetry and Fourier Transform Infrared Spectroscopy indicated that the drug and excipients were compatible and the drug was encapsulated into nanoparticles. The comparison of drug release profiles demonstrated that drug release from nanoparticles prepared with both higher molecular weight and higher concentration polymers decelerated but the drug release accelerated as the amount of glycolide in the copolymer composition increased. Weibull kinetic model was found to fit best for OND release from PLGA-PNPs. The cytotoxicity effect of the pure drug, marketed drug (Zofer (R)), and optimized formulations were tested in the L929 cell line, and the results exhibited that the cell viability of optimized pegylated formulation was higher than 90% after 48 h of incubation.

Abstract This study aims to develop a multifunctional liposomal radiosensitizer to destroy more tumor cells by using lower radiation doses compared to clinically used 6 MV X-ray doses. To achieve this aim, first Chlorine-e6 (Ce6) was covalently bound to functional groups of outer surfaces of quantum dots (QDs) through EDC/NHS reactions. Then, QDs-Ce6 conjugate loaded, nanosized, PEG-coated, and tumor-specific folic acid-modified immunoliposome dispersions were prepared by film method. Enhanced anti-proliferation activity of free and liposomal conjugate against 4T1 (murine breast cancer) cell lines was investigated at different X-ray doses (5, 10, 15, and 20 Gy). As a result, the best radiosensitizer effect was observed at a 5 Gy X-ray dose and it was found that following the X-ray irradiation, immunoliposome dispersions containing QDs-Ce6 conjugate killed 26.8 ± 1.7% more cancer cells than radiation alone.

Furosemide is a widely used diuretic drug for the treatment of edema associated with heart, liver cirrhosis, renal diseases and hypertension. It is a Class IV drug with low aqueous solubility and low permeability according to Biopharmaceutics Classification System (BCS). Furosemide was chosen as a model drug to examine the effect of polymeric precipitation inhibitors (PPIs) on the supersaturation and solubility. Solubility and concentration change of furosemide as a function of time at pH 1.2 and 6.8 were determined to show the effects of PPIs on furosemide solubility. The 24 h equilibrium solubility of furosemide was 0.017 +/- 0.004 and 3.62 +/- 0.201 mg/mL at pH 1.2 and pH 6.8 buffer solutions, respectively. PPI type and concentration (0.05%, 0.25%) did not increase furosemide solubility at pH 1.2. However, both hydroxypropylmethylcellulose (HPMC) and polyvinylpyrrolidoneK17 (PVPK17) at two concentrations increased furosemide solubility at pH 1.2 and 6.8. In addition, viscosity of solutions was in the range of 2.2-3.7 centipoise, and it was not influenced by PPIs concentrations. Our results showed that designing supersaturated formulations using PPIs can be useful and promising to enhance solubility of furosemide.

Nanoparticles are advantageous systems due to unique properties they present when they are used as drug delivery systems. One of the most intriguing approaches to obtain a desirable in vivo fate for nanoparticles is designing stimuli-responsive nanoparticles. Stimuli-responsive behavior can be obtained by using stimuli-responsive materials for forming of nanoparticles. Nanocarriers lead to some adverse effects, including uncontrollable drug release and biodistribution, because of some intracellular and extracellular barriers. In clinical use controlled-release nanosized drug delivery systems are present, but many of these controlled-release systems offer either constant or decreasing drug release and they are not sensitive to changes in the body that occur due to pathologies or external stimuli. Local abundance of enzymes at the tumor site is thought to provide drug release at the desired site, while in normal tissues low expression of enzymes is considered insufficient to cause drug release.

Nanoparticles are suitable delivery systems for targeting of drugs, and extensive research in the field of nanomedicine is ongoing. Apart from cellular uptake, nanoparticles sometimes have to cross cellular barriers. Understanding the cellular uptake and transcytosis of nanoparticles are crucial for designing efficient nanoparticles. This chapter provides a review of cellular uptake mechanisms and transcytosis of nanoparticles. Also, the effect of the physicochemical characteristics of nanoparticles on their cellular internalization is also discussed. Although nanocarriers sometimes release their payload at the extracellular disease site and the released active ingredient enters the cells by itself to show its effect, another way is to deliver nanoparticles directly into cells, and then the payload is released there and it shows its effect. Electrostatic, van der Waals, and ionic forces between the cell and the nanoparticle and receptor-mediated recognition of opsonins are behind phagocytosis of nanoparticles.

Here we present self-assembled polymeric micelles as potential delivery systems for therapeutic agents with highly tunable properties.

Purpose: The aim of this study was to design naproxen sodium (NS)-containing, biomimetic, porous poly(lactide-co-glycolide) (PLGA) scaffolds for regeneration of damaged corneal epithelium. Methods: NS-incorporated PLGA scaffolds were prepared using the emulsion freeze-drying method and then coated with collagen or poly-l-lysine. Porosity measurements of the scaffolds were performed by the gas adsorption/desorption method and the scaffolds demonstrated highly porous, open-cellular pore structures with pore sizes from 150 to 200 mu m. Results: The drug loading efficiency of scaffolds was found to be higher than 84%, and about 90%-98% of NS was released at the end of 7 days with a fast drug release rate at the initial period of time and then in a slow and sustained manner. The corneal epithelial cells were isolated from New Zealand white rabbits. The obtained cells were seeded onto scaffolds and continued to increase during the time period of the study, indicating that the scaffolds might promote corneal epithelial cell proliferation without causing toxic effects for at least 10 days. Conclusions: The NS-loaded PLGA scaffolds exhibited a combination of controlled drug release and biomimetic properties that might be attractive for use in treatment of corneal damage both for controlled release and biomedical applications.