The localized delivery of fluconazole (FLZ) by conventional therapy is a major impediment in achieving its therapeutic efficacy against skin infections, such as cutaneous candidiasis. Therefore, the present study was aimed to develop FLZ-loaded vesicular construct(s), such as liposomes and niosomes, incorporated into carbopol gel (1%; w/w) for sustained, localized application. The liposomes and niosomes were prepared by the lipid/nonionic surfactant-based dry-film hydration method and were characterized for different parameters. In addition, antifungal activity was carried out on experimentally induced cutaneous candidiasis in immunosuppressed albino rats. The results showed that the size of liposomes and niosomes was found to be 0.348 ± 0.054 and 0.326 ± 0.033 μm with encapsulation efficiency of 31.8 ± 1.36 and 27.6 ± 1.08%, respectively. The skin-retention studies of FLZ from in vitro and in vivo experiments showed significantly higher accumulation of drug in the case of liposomal gel. The in vivo localization studies in viable skin showed that liposomal gel could produce 14.2-fold higher drug accumulation, compared with plain gel, while it was 3.3-fold more in the case of an equivalent-dose application in the form of niosomal gel. The antifungal study also confirmed the maximum therapeutic efficacy of liposomal gel, as the lowest number of cfu/mL was recorded following liposomal FLZ application. The studies signify the potential of liposomal gel for topical delivery of FLZ with increased accumulation of drug in various strata of skin vis-a-vis through sustained release of drug could maintain the localized effect, resulting in an effective treatment of a life-threatening cutaneous fungal infection.
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http://dx.doi.org/10.3109/08982101003596125 | DOI Listing |
Pharmaceutics
November 2024
Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou 570228, China.
: Lung cancer is an aggressive disease with rapid progression and a high rate of metastasis, leading to a significantly poor prognosis for many patients. While chemotherapy continues to serve as a cornerstone treatment for a large proportion of lung cancer patients, expanding preclinical and clinical evidence indicates that chemotherapy may promote tumor metastasis and cause side effects. : We develop an injectable bait-and-hook hydrogel (BH-gel) for targeted tumor cell eradication, which embedded doxorubicin liposomes as cytotoxic agents and CXCL12 as a chemoattractant to capture and kill tumor cells.
View Article and Find Full Text PDFInt J Pharm
December 2024
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, Egypt.
Oleic acid liposomes (OALs) are novel vesicular carriers ofunsaturated fatty acids and their corresponding ionized species, arranged within an enclosed lipid bilayer. This study aimed to encapsulate moxifloxacin HCl (MOX), a broad-spectrum antibacterial drug into OALs for effective treatment of Methicillin-resistant Staphylococcus aureus (MRSA) infection through topical application. Various OALs were formulatedby combining varied quantities of phosphatidylcholine (PC), oleic acid (OA), and cholesterol (CH) with 50 mg of MOX.
View Article and Find Full Text PDFMethods Mol Biol
December 2024
Heidelberg University Biochemistry Center, Heidelberg, Germany.
Functionalized lipid analogs are a versatile tool for studying lipid localization, metabolism and interactions in cells. As a common follow-up research, in vitro experiments are utilized to confirm specific interactors and characterize protein-lipid interactions. Here, we describe protocols that rely on commercially available photoactivatable and clickable lipids in reconstituted systems to capture protein-lipid interactions and detect lipid transport between purified proteins.
View Article and Find Full Text PDFInt J Pharm
January 2025
Department of Obstetrics and Gynecology, Duke University Medical Center, Durham, NC 27710; Department of Chemistry and Biochemistry, North Carolina Central University, Durham, NC 27707. Electronic address:
Recent Adv Drug Deliv Formul
December 2024
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11884, Egypt.
Background: Norfloxacin (NFX) is a wide-spectrum antibacterial agent that suffers from low water solubility and first-pass metabolism. This diminishes its oral bioavailability by 60-70%.
Objective: This work aims to formulate a topical gel of NFX-loaded lipid polymer hybrid nanoparticles (NFX-LPHNPs) that combine the merits of liposomes and polymeric nanoparticles to overcome these problems.
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