Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

Bolla, Pradeep Kumar; Meraz, Carlos Alberto; Rodriguez, Victor A.; Deaguero, Isaac G.; Singh, Mahima; Yellepeddi, Venkata K.; Renukuntla, Jwala

doi:10.3390/molecules24173139

Cited by 55 publications

(46 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The characteristic endothermic peak of lutein disappeared in thermograms of lutein-loaded polymeric nanoparticles, suggesting that lutein was rendered amorphous by its interaction with the polymer. The transformation of lutein from crystalline to amorphous form is important, as amorphous forms are characterized by higher solubilities and increased bioavailability [ 51 , 52 , 53 , 54 ]. Similar results (loss of characteristic peak) were observed in other studies where crystalline drugs such as SN-38, doxorubicin oxcarbazepine, prilocaine, and adefovir were encapsulated into PLGA-based micro- and nanoparticles [ 24 , 25 , 55 , 56 , 57 ].…”

Section: Resultsmentioning

confidence: 99%

Lutein-Loaded, Biotin-Decorated Polymeric Nanoparticles Enhance Lutein Uptake in Retinal Cells

et al. 2020

Self Cite

View full text Add to dashboard Cite

Age related macular degeneration (AMD) is one of the leading causes of visual loss and is responsible for approximately 9% of global blindness. It is a progressive eye disorder seen in elderly people (>65 years) mainly affecting the macula. Lutein, a carotenoid, is an antioxidant, and has shown neuroprotective properties in the retina. However, lutein has poor bioavailability owing to poor aqueous solubility. Drug delivery to the posterior segment of the eye is challenging due to the blood–retina barrier. Retinal pigment epithelium (RPE) expresses the sodium-dependent multivitamin transporter (SMVT) transport system which selectively uptakes biotin by active transport. In this study, we aimed to enhance lutein uptake into retinal cells using PLGA–PEG–biotin nanoparticles. Lutein loaded polymeric nanoparticles were prepared using O/W solvent-evaporation method. Particle size and zeta potential (ZP) were determined using Malvern Zetasizer. Other characterizations included differential scanning calorimetry, FTIR, and in-vitro release studies. In-vitro uptake and cytotoxicity studies were conducted in ARPE-19 cells using flow cytometry and confocal microscopy. Lutein was successfully encapsulated into PLGA and PLGA–PEG–biotin nanoparticles (<250 nm) with uniform size distribution and high ZP. The entrapment efficiency of lutein was ≈56% and ≈75% for lutein-loaded PLGA and PLGA–PEG–biotin nanoparticles, respectively. FTIR and DSC confirmed encapsulation of lutein into nanoparticles. Cellular uptake studies in ARPE-19 cells confirmed a higher uptake of lutein with PLGA–PEG–biotin nanoparticles compared to PLGA nanoparticles and lutein alone. In vitro cytotoxicity results confirmed that the nanoparticles were safe, effective, and non-toxic. Findings from this study suggest that lutein-loaded PLGA–PEG–biotin nanoparticles can be potentially used for treatment of AMD for higher lutein uptake.

show abstract

Section: Resultsmentioning

confidence: 99%

Lutein-Loaded, Biotin-Decorated Polymeric Nanoparticles Enhance Lutein Uptake in Retinal Cells

et al. 2020

Self Cite

View full text Add to dashboard Cite

show abstract

“…Miconazole loaded nano-vesicles were prepared by using a thin-film hydration method previously used in a similar azole study [ 15 ]. Miconazole, cholesterol, and sodium oleate were dissolved in 10 mL of methanol and chloroform in a 1:1 ratio solution.…”

Section: Methodsmentioning

confidence: 99%

“…Lipid encapsulation has been shown to enhance delivery while also increasing the efficacy of antifungal drugs [ 14 ]. Previous studies involving the use of a combination of cholesterol and sodium oleate with proper ratios have been successful in transdermal drug delivery, while maintaining respectable drug encapsulation efficiency [ 15 ]. Understanding the proper ratios of miconazole, cholesterol, and sodium oleate, as well as measuring vesicle size, polydispersity index, zeta potential, and encapsulation efficiency are paramount to understanding overall drug efficacy, and were intimately studied to ensure that the best combination to battle infection would be properly utilized for further study.…”

Section: Introductionmentioning

confidence: 99%

Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro

et al. 2020

View full text Add to dashboard Cite

Opportunistic fungal infections are responsible for over 1.5 million deaths per year. This has created a need for highly effective antifungal medication to be as potent as possible. In this study, we improved the efficacy of a common over the counter (OTC) antifungal skin medication, miconazole, by encapsulating nano-molecules of the drug in cholesterol/sodium oleate nano-vesicles. These nano-vesicles were characterized to optimize their size, zeta potential, polydispersity index and encapsulation efficiency. Furthermore, these nano-vesicles were compared to a conventional miconazole-based commercially available cream to determine potential improvements via permeation through the stratum corneum, cytotoxicity, and antifungal capabilities. Our results found that the vesicle size was within the nano range (~300 nm), with moderate polydispersity and stability. When compared with the commercially available cream, Actavis, as well as free miconazole, the miconazole nano-vesicle formulation displayed enhanced fungal inhibition by a factor of three or more when compared to free miconazole. Furthermore, with smaller nanoparticle (NP) sizes, higher percentages of miconazole may be delivered, further enhancing the efficacy of miconazole’s antifungal capability. Cytotoxicity studies conducted with human dermal fibroblast cells confirm its biosafety and biocompatibility, as cell survival rate was observed to be twofold higher in nano-vesicle formulation than free miconazole. This formulation has the potential to treat fungal infections through increasing the retention time in the skin, improving the treatment approach, and by enhancing the efficacy via the use of nano-vesicles.

show abstract

“…Topical/transdermal drug delivery refers to the delivery of drugs via skin and is an attractive alternative to conventional methods such as oral and parenteral routes. Advantages associated with topical/transdermal delivery include non-invasive delivery, bypass of first pass metabolism, prolonged duration of action, reduced dosing frequency, constant levels of drug in the plasma, reduced drug toxicity/adverse events, improved patient compliance, and others [1][2][3]. However, skin acts as a major barrier for the entry of drugs and foreign compounds due to the presence of stratum corneum, a thin keratin-rich layer (15 µm) of dead cells embedded in an intricate lipid environment made of cholesterol, ceramides, and free fatty acids [4][5][6].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Formulation Parameters on Permeation of Ibuprofen from Topical Formulations Using Strat-M® Membrane

et al. 2020

Self Cite

View full text Add to dashboard Cite

Topical drug delivery is an attractive alternative to conventional methods because of advantages such as non-invasive delivery, by-pass of first pass metabolism, and improved patient compliance. However, several factors such as skin, physicochemical properties of the drug, and vehicle characteristics influence the permeation. Within a formulation, critical factors such as concentration of drug, physical state of drug in the formulation, and organoleptic properties affect the flux across the skin. The aim of the study was to develop and investigate topical semisolid preparations (creams and gels) with ibuprofen as the model drug and investigate the effect of various formulation parameters on the in-vitro performance across the Strat-M® membrane using flow-through cells. In addition, the physical stability of the developed formulations was investigated by studying viscosity, pH, and appearance. All the formulations developed in the study had appealing appearance with smooth texture and no signs of separation. Viscosity and pH of the formulations were acceptable. Cumulative amount of drug permeated at the end of 24 h was highest for clear gel (3% w/w ibuprofen; F6: 739.6 ± 36.1 µg/cm2) followed by cream with high concentration of ibuprofen in suspended form (5% w/w; F3: 320.8 ± 17.53 µg/cm2), emulgel (3% w/w ibuprofen; F5: 178.5 ± 34.5 µg/cm2), and cream with solubilized ibuprofen (3% w/w; F2A: 163.2 ± 9.36 µg/cm2). Results from this study showed that permeation of ibuprofen was significantly influenced by formulation parameters such as concentration of ibuprofen (3% vs. 5% w/w), physical state of ibuprofen (solubilized vs. suspended), formulation type (cream vs. gel), mucoadhesive agents, and viscosity (high vs. low). Thus, findings from this study indicate that pharmaceutical formulation scientists should explore these critical factors during the early development of any new topical drug product in order to meet pre-determined quality target product profile.

show abstract

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

Cited by 55 publications

References 47 publications

Lutein-Loaded, Biotin-Decorated Polymeric Nanoparticles Enhance Lutein Uptake in Retinal Cells

Lutein-Loaded, Biotin-Decorated Polymeric Nanoparticles Enhance Lutein Uptake in Retinal Cells

Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro

Evaluation of Formulation Parameters on Permeation of Ibuprofen from Topical Formulations Using Strat-M® Membrane

Contact Info

Product

Resources

About