Neda Bavarsad

This study aimed to develop an oral succinyl chitosan-coated liposomal formulation containing grape seed extract and assess its therapeutic efficacy in rats with bleomycin-induced pulmonary fibrosis. N-succinyl chitosan was synthesized, and the liposomal formulations were prepared and characterized regarding phenolic content assay and morphology. Size, zeta potential, in vitro drug release, and stability. Pulmonary fibrosis was induced by intratracheal bleomycin injection, and hydroxyproline measurements, lung weight, animal body weight, as well as histopathological studies were performed Succinyl chitosan increases the physical stability of the formulation, especially in acidic conditions. Drug release studies revealed that 66.27% of the loaded drug was released from CF2 in an acidic medium in 2 hr, but 92.31% of the drug was released in 8 hr in a pH=7 medium. An in vivo study demonstrated that rats exposed to bleomycin significantly lost weight, while those treated with CF2 (400 mg/kg) partially regained weight. Bleomycin treatment increased the mean lung weight and the amount of hydroxyproline in the lungs; these values were significantly decreased in the group treated with 400 mg/kg CF2 (P <0.05). Histopathological examination confirmed that treatment with 400 mg/kg CF2 improved lung fibrosis. In rats, oral administration of N-succinyl chitosan-coated liposomes containing grape seed extract at the 400 mg/kg dose ameliorates bleomycin-induced pulmonary fibrosis.

The present study aimed to formulate and characterize mucoadhesive liposomes for intranasal delivery of loratadine. In particular, the formulation was aimed to improve the drug bioavailability and efficacy. Liposomes were prepared by thin-film hydration method, with soybean phosphatidylcholine and cholesterol as main components. Liposomes were coated with chitosan solution at a concentration of 0.05% and 0.1%, w/v. The formulations were assessed for particle size, polydispersity index (PDI), encapsulation efficiency (EE), thermodynamic behavior, in vitro drug release, mucoadhesiveness, and stability. Particle size analysis showed that the vesicles of uncoated and coated liposomes with 0.05% and 0.1% chitosan were characterized by size of 193±3.3 nm, 345±4.6, and 438±7.3 nm, respectively. Size distribution for developed formulations was in the acceptable range (PDI 0.05). For stability studies, liposomes were stored at 4°C for 3 months, and changes in particle diameter, PDI, and EE % were recorded. No significant alternations were reported in particles size, PDI, and drug leakage of coated liposomes. Liposomes coated with 0.05% chitosan were chosen as the optimum formulation, which demonstrated a significant potential for overcoming the nasal drug delivery limits for short residence time and mucociliary clearance.

Objective: Melasma is an acquired hyperpigmentation disorder, and reactive oxygen species play important role in regulating melanin synthesis. Lycopene is one of the most effective oxygen neutralizers among tomato‐derived carotenoids. Also, hydroquinone is a compound that has been used for the treatment of hyperpigmentation by mechanism of tyrosinase inhibition and can be found in wheat.Methods: An appropriate cream formulation containing 0.05% tomato lycopene and 3.45% wheat bran extract was prepared, and physicochemical characterization was performed. The prepared formulations were applied twice a day for three months in combination with SPF = 30 sunscreen by 22 patients diagnosed with melasma. MASI score in two groups was evaluated at weeks 0, 3, 6, 9, and 12 and 1 month after the treatment.Results: The prepared formulation shows smooth and homogeneous appearance with suitable spreadability and viscosity. The MASI score of intervention group from the sixth week until the end of the treatment was significantly decreased compared to the onset of the treatment (P < .05), and the mean difference of the MASI score and the rate of skin discoloration in intervention group (0.53 ± 0.47 and 3.73 ± 1.90, respectively) were significantly higher than in placebo group (0.14 ± 0.20 and 0.91 ± 0.07, respectively; P < .05). Size of melasma during the study was decreased significantly from 6.59 ± 3.47 to 5.97 ± 3.83 (P < .05).Conclusion: The data of mean difference of the MASI score indicated skin improvement in intervention group. Meanwhile, no recurrence was observed one month after the end of the treatment. These data suggest that the prepared formulation containing lycopene and wheat bran extract is safe and could be promising as an efficacious cosmetic treatment.

The aim of this study was to develop and optimize deformable liposome for topical delivery of tretinoin. Liposomal formulations were designed based on the

Keywords: Dermal Applications; Particles, Lipid

Dorzolamide ophthalmic drop is one of the most common glaucoma medications but it has a short residence time in the eye. The aim of this study is to develop ocular dorzolamide HCl nanoliposomes (DRZ - nanoliposomes) and to evaluate their potential use for the treatment of ocular hypertension. Nanoliposomes were prepared using Reverse-phase evaporation vesicle (REV) and thin layer hydration (TLH) method with 7:3 and 7:4 molar ratios of phosphatidylcholine:cholesterol. The physicochemical properties of the formulations were investigated. Formulations with 7:4 lipid ratios were evaluated in terms of drug release, physical stability and ex-vivo permeation through the excised albino rabbit cornea. The rabbits in groups of 6 were treated with selected DRZ - nanoliposomes or dorzolamide solution or marketed dorzolamid preparation (Biosopt®) and intraocular pressure (IOP) was monitored. Formulations with 7:4 molar ratio entrapped greater amount of drug compared to those with 7:3 lipid components ratio. DRZ - nanoliposomes with 7:4 lipid ratio showed more transcorneal permeation than Dorzolamide solution (p<0.05); and the formulation prepared by TLH method exhibited higher permeability than that prepared by REV method (p<0.05). The selected DRZ - nanoliposomes showed greater IOP lowering activity and a more prolonged effect compared to dorzolamide solution and Biosopt®. DRZ - nanoliposomes prepared by TLH method with 7:4 ratios showed promising results as a candidate for the treatment of ocular hypertension.

Griseofulvin is an antifungal drug and is available as oral dosage forms. Development of topical treatment could be advantageous for superficial fungal infections of the skin. In this study, films prepared from the incorporation of griseofulvin-loaded liposomes in chitosan film for topical drug delivery in superficial fungal infections. The properties of the films were characterized regarding mechanical properties, swelling, ability to transmit vapor, drug release, thermal behavior, and antifungal efficacy against Microsporum gypseum and Epidermophyton floccosum. The presence of liposomes led to decreased mechanical properties but lower swelling ratio. Higher amount of drug permeation and rate of flux were obtained by liposomes incorporated in films compared to liposomal formulations. Antifungal efficacy of formulations was confirmed against two species of dermatophytes in vitro. Therefore, two concepts of using vesicular carrier systems and biopolymeric films have been combined and this topical novel composite film has the potential for griseofulvin delivery to superficial fungal infections.