Multilamellar liposomes of triamcinolone acetonide: preparation, stability, and characterization

Clares, Beatriz; Gallardo, V.; Medina, Mariano Montilla; Ruíz, M. A.

doi:10.1080/08982100902736571

Cited by 17 publications

(8 citation statements)

References 28 publications

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“…Student t-test shows that there is a significant difference between liposomal formulations of the same molar ratio after and before incorporation of atocopherol acetate at a = 0.05. The increase in the entrapment efficiency is explained by the fact that incorporation of atocopherol acetate into liposomal preparations improves the membrane rigidity and makes it more hydrophobic and less permeable (Clares et al, 2009). Moreover a reduction in the lipid peroxidation and decrease in the formation of lysophospholipid occur when tocopherol is added.…”

Section: Drug Entrapment Efficiencymentioning

confidence: 94%

Effect of formulation design and freeze-drying on properties of fluconazole multilamellar liposomes

El-Nesr

Yahiya

El‐Gazayerly

2010

Saudi Pharmaceutical Journal

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Fluconazole-entrapped multilamellar liposomes were prepared using the thin-film hydration method. The effects of cholesterol molar ratio, charge-inducing agents, and α-tocopherol acetate on encapsulation efficiency values and in vitro drug release of multilamellar liposomes were studied. Freeze-dried liposomal products were prepared with or without cryoprotectants. Results showed that incorporation of stearylamine resulted in an increased entrapment of fluconazole, whereas incorporation of dicetyl phosphate decreased the drug entrapment efficiency. The incorporation of α-tocopherol acetate into fluconazole multilamellar liposomes resulted in the increase of entrapment efficiency of fluconazole liposomes. In vitro release studies revealed that incorporation of cholesterol into multilamellar liposomal formulations decreased drug permeability from formulations. Positively charged fluconazole multilamellar liposomes gave rise to a slow release rate compared to neutral liposomes whereas negatively charged fluconazole liposomes showed a rapid release rate. Physical stability studies showed that lyophilized cake of liposomes without cryoprotectants was compact and difficult to reconstitute compared to fluffy easily reconstituted cakes upon using cryoprotectants. Fluconazole retained in freeze-dried liposomes without cryoprotectants was 63.452% compared to 91.877% using three grams of trehalose as a cryoprotectant per gram lipid in positively charged multilamellar liposomes. Physical stability studies showed superior potentials of the lyophilized product after reconstitution in comparison with those of a solution product.

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Section: Drug Entrapment Efficiencymentioning

confidence: 94%

Effect of formulation design and freeze-drying on properties of fluconazole multilamellar liposomes

El-Nesr

Yahiya

El‐Gazayerly

2010

Saudi Pharmaceutical Journal

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“…Lipid based nanoparticulate systems have shown promising results in enhancing drug permeation across anatomical tissues, thus increasing overall efficacy [10,11]. Attempts have been made by various researchers to formulate TA topically in the form of aqueous nanomicellar drops [12], liposomes [13,14], and NLCs [4,5]. The results, however, in terms of drug loading and ocular tissue TA concentrations are either not promising or are lacking.…”

Section: Introductionmentioning

confidence: 99%

In Situ Gel of Triamcinolone Acetonide-Loaded Solid Lipid Nanoparticles for Improved Topical Ocular Delivery: Tear Kinetics and Ocular Disposition Studies

et al. 2018

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Triamcinolone acetonide (TA), an intermediate acting corticosteroid, is used in the treatment of posterior ocular diseases, such as inflammation, posterior uveitis, and diabetic macular edema. The objective of this investigation was to prepare TA-loaded solid lipid nanoparticles (TA-SLNs) and in situ gel (TA-SLN-IG) formulations for delivery into the deeper ocular tissues through the topical route. TA-SLNs were prepared by hot homogenization and ultrasonication method using glyceryl monostearate and Compritol® 888ATO as solid lipids and Tween®80 and Pluronic® F-68 as surfactants. TA-SLNs were optimized and converted to TA-SLN-IG by the inclusion of gellan gum and evaluated for their rheological properties. In vitro transcorneal permeability and in vivo ocular distribution of the TA-SLNs and TA-SLN-IG were studied using isolated rabbit corneas and New Zealand albino rabbits, respectively, and compared with TA suspension, used as control (TA-C). Particle size, PDI, zeta potential, assay, and entrapment efficiency of TA-SLNs were in the range of 200–350 nm, 0.3–0.45, −52.31 to −64.35 mV, 70–98%, and 97–99%, respectively. TA-SLN-IG with 0.3% gellan gum exhibited better rheological properties. The transcorneal permeability of TA-SLN and TA-SLN-IG was 10.2 and 9.3-folds higher compared to TA-C. TA-SLN-IG showed maximum tear concentration at 2 h, indicating an improved pre-corneal residence time, as well as higher concentrations in aqueous humor, vitreous humor and cornea at 6 h, suggesting sustained delivery of the drug into the anterior and posterior segment ocular tissues, when compared to TA-SLN and TA-C. The results, therefore, demonstrate that the lipid based nanoparticulate system combined with the in situ gelling agents can be a promising drug delivery platform for the deeper ocular tissues.

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“…Therefore a proper understanding of the molecular interactions as a function of the liposomal membrane composition is a prerequisite for efficient encapsulation and optimum release outcomes [21]. Despite these well-recognized effects of cholesterol in conventional liposomal formulations, recent research also focuses on low cholesterol or cholesterolfree liposomes for entrapment of hydrophobic molecules such as idarubicin [23], paclitaxel [24], nystatin [25], tamoxifen [26] and triamcinolone acetonide [27]. Despite these well-recognized effects of cholesterol in conventional liposomal formulations, recent research also focuses on low cholesterol or cholesterolfree liposomes for entrapment of hydrophobic molecules such as idarubicin [23], paclitaxel [24], nystatin [25], tamoxifen [26] and triamcinolone acetonide [27].…”

Section: Introductionmentioning

confidence: 99%

Celecoxib-loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics

et al. 2010

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CLX (celecoxib) is a highly hydrophobic non-steroidal anti-inflammatory drug with high plasma protein binding. We describe here the encapsulation of CLX in MLVs (multilamellar vesicles) composed of DSPC (1,2-distearoyl-sn-glycero-3-phosphocholine) and variable amounts of cholesterol. The effects of cholesterol content on liposome size, percentage drug loading and in vitro drug release profiles were investigated. Differential scanning calorimetry and FTIR (Fourier-transform infrared) spectroscopy were used to determine molecular interactions between CLX, cholesterol and DSPC. The phase transition temperature (Tm) of vesicles was reduced in a synergistic manner in the presence of both CLX and cholesterol. Encapsulation efficiency, loading and release of CLX decreased with increasing cholesterol content. FTIR results indicated that this decrease was due to a competition between CLX and cholesterol for the co-operativity region of the phospholipids. In the presence of cholesterol, CLX was pushed further into the hydrophobic core of the bilayer. However, MLVs prepared with DSPC only (without cholesterol) exhibited the lowest ability for drug retention after 72 h. Our results indicated that CLX, without the requirement of modifications to enhance solubilization, can be encapsulated and released from liposomal formulations. This method of drug delivery may be used to circumvent the low bioavailability and systemic side effects of oral CLX formulations.

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Multilamellar liposomes of triamcinolone acetonide: preparation, stability, and characterization

Cited by 17 publications

References 28 publications

Effect of formulation design and freeze-drying on properties of fluconazole multilamellar liposomes

Effect of formulation design and freeze-drying on properties of fluconazole multilamellar liposomes

In Situ Gel of Triamcinolone Acetonide-Loaded Solid Lipid Nanoparticles for Improved Topical Ocular Delivery: Tear Kinetics and Ocular Disposition Studies

Celecoxib-loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics

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