Objectives: In this study, we aimed to incorporate levocetirizine dihydrochloride (LVC) into electrospun nanovesicle-in-nanofiber (NF) scaffolds for combined management of atopic dermatitis and methicillin-resistant Staphylococcus Aureus skin infection, to sustain LVC release for continuous skin improvement. Methods: Firstly, LVC was encapsulated in cerosomes (CERs) by employing a thin-film hydration approach using a 2¹.3¹ factorial design. CERs were assessed by calculating entrapment efficiency (EE%), particle size (PS) and polydispersity index (PDI). In addition, the optimized CERs were further subjected to stability evaluation. After that, the optimized CERs were incorporated into polyurethane nanofibers (NFs) using a coaxial electrospinning technique. An in vitro release assay was used to calculate the amount of LVC released from the LVC-NFs and the optimized CERs-NFs. For morphological assessment of NFs, LVC-NFs and CERs-NFs were subjected to transmission electron microscopy, scanning electron microscopy, and confocal laser scanning microscopy. Atomic force microscopy was utilized to evaluate the roughness of CERs and both NFs. The optimum formulation was further subjected to in vivo study. Results: The optimum CERs exhibited an EE% of 65.03 ± 1.07%, a PS of 680.00 ± 39.50 nm, and a PDI of 0.51 ± 0.04. LVC was released in a sustained manner from CERs NFs. Further, a dermatokinetic study confirmed that CERs-NFs sustained the infiltration of LVC, compared with the other groups. Finally, a safety assessment showed that all formulations were safe when topically applied to rat skin. Conclusions: In conclusion, AD and MRSA skin infections may be cured by employing electrospun nanofiber-scaffold-loaded LVC CERs, which can thus be regarded as a promising system.

Background: Bilosomes are vesicular nanocarriers that contain bile salts, making them more flexible and resistant to degradation in the gastrointestinal tract. Objective: To evaluate the effect of two bile salts on the physical properties and stability of the ropinirole-loading bilosome. Methods: Sixteen bilosomal formulations were prepared by a reverse-phase evaporation method. Each formula includes a mixture of non-ionic surfactants (Span®60 and Tween®60), along with cholesterol and bile salts (either sodium taurocholate (STC) or sodium glycocholate (SGC). The characteristics of the bilosomal formulations (drug content, entrapment efficiency, vesicle size, polydispersity index, zeta potential, in-vitro drug release, and Fourier transform infrared spectroscopy) were evaluated. Results: The entrapment efficiency of ropinirole was reduced by using sodium glycocholate instead of sodium taurocholate. The vesicle size and zeta potential were also affected by the type of bile salt and its amount. Drug release profiles were sustained, indicating a good entrapment of ropinirole. The STC-containing bilosomes are more stable than the SGC-containing bilosomes. Bilosomal formula F5 showed the highest entrapment efficiency (64.82%), suitable vesicle size (179.8 nm), zeta potential (-9.162 mV), polydispersity index (0.5116), and in vitro drug release (62.33%) after 24 hr. Conclusion: Sodium taurocholate was more suitable for the preparation of ropinirole-loading bilosomes, with more stability of bilosomes in bile salt solution.

Background: Ropinirole hydrochloride is a non-ergoline antiparkinson drug. It is a highly hydrophilic drug and classified as class III according to Biopharmaceutical Classification System with low absolute oral bioavailability of approximately 50% upon oral administration due to significant hepatic first-pass metabolism. Objective: to compare the pharmacokinetic parameters of Ropinirole when administered orally in the form of an Ropinirole bilosomal dispersion in contrast to an oral Ropinirole solution. Methods: This study involved the use of twelve male Wistar rats, with an average weight of 220±11 g, and these rats were divided into two groups, comprising six rats each. A 1.1 mg/kg doses of pure Ropinirole and Ropinirole bilosomes were administered orally through gavage after reconstituting in distilled water. Ropinirole was quantified in the rat's plasma using HPLC, subsequently establishing a spiked calibration curve with plasma samples and utilizing paracetamol as an internal standard. The statistics included mean values (± SD; n = 6) for pharmacokinetic parameters, with statistical significance assessed using a student's t-test. Results: For the oral bilosomes, the values were 9.4±0.11 μg /ml for Cmax, 3±0.00 h for Tmax, and 55.56±2.12 μg h/ml for AUC0-24. In contrast, for the oral solution, the corresponding values were 7.2±0.14 μg/ml for Cmax, 1.5±0.00 h for Tmax, and 23.70±2.23 μg h/ml for AUC0-24. These parameters were significantly higher (P<0.05) as compared with a pure drug solution. The comparative bioavailability of Ropinirole (AUC0-24 oral solution / AUC0-24 oral bilosomes ) is equal to 42.66%, which indicates the bioavailability of the oral RH solution was less than that of RH bilosomal dispersion. Conclusions: The use of nanovesicular carriers (bilosomes) shows significant potential as an effective delivery system for improving the oral bioavailability of ropinirole hydrochloride.

Objective: The current investigation aimed for loading Lidocaine (LID), a local anesthetic agent, into transferosomes topically. Lidocaine has substantial first-pass metabolism results in low oral bioavailability. In order to prevent oral complications, the production of LID transferosomes was to improve LID topical distribution. Methods: By using a 21.31 factorial design and different amounts lipids and surfactants, transferosomes formulas were created. LID transferosomes were constructed applying ethanol injection method. LID transferosomes were evaluated with regard to entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). Extra experiments were conducted on the optimum formula. Results: Utilizing Design Expert®, the optimum formula (F2) was evaluated, revealing EE% of 90.25±1.23%, PS of 194.50±6.50 nm, PDI of 0.602±0.0005, ZP of 50.45±1.15 mV, and amount of drug release after 6 h (Q6h) of 45.00±1.50. Further, the optimum transferosomes showed vesicles without aggregation under transmission electron microscope evaluation. In vitro release study showed that the optimum formula was released in sustained manner than LID solution. In addition, during storage, the optimum formula was stable. The histological investigation verified the safety of the optimum transferosomes. Conclusion: The results confirmed the ability to utilize LID transferosomes for burn treatment topically.

Parsley leaves (Petroselinum crispum) biennial herb native to the Mediterranean has diverse bioactive phytochemicals, like flavonoids and phenolic acids that known for their potent antioxidant and cytotoxic properties. This study aimed to isolate two phenolic compounds, Apigenin and Syringic acid from ethyl acetate fraction of parsley leaves extract and evaluate their cytotoxic activity against A375 cell line compared to normal cells. Ultrasonication was used to extract the active compounds using 90% ethanol, and PHPLC was used to isolate the two phenolic compounds. FT-IR was used to categorize the active functional groups comprising the two isolated phenolic compounds. The results showed the isolation of syringic acid and apigenin, apigenin exhibited cytotoxic activity with IC50% 40.8 µg /ml and Syringic acid exhibited cytotoxic activity with IC50 values 54.5 µg /ml, Apigenin showing a stronger cytotoxic activity than Syringic acid. Both isolated phenolic compounds exhibited strong cytotoxic activity depend on increasing concentration of each compound, and Apigenin showing particularly high cytotoxic activity against A375 cell line.