The influence of particle size of liposomes on the deposition of drug into skin

Plessis, Jeanetta du; Ramachandran, Chandrasekharan; Weiner, Norman; Müller, D.G.

doi:10.1016/0378-5173(94)90178-3

Cited by 175 publications

(77 citation statements)

References 13 publications

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“…Contrary to the previous findings, Du Plessis et al (1994b), who studied the effect of particle size of liposomes on the skin deposition of ciclosporin, found that the intermediate size and not the small size entities resulted in higher amounts. They considered this as an indication that intact liposomes did not penetrate the skin; if such input operated, better results should be obtained as the particle size decreased.…”

Section: Free Drug Mechanism (See Figure 3 At A)contrasting

confidence: 47%

Untitled

2006

Journal of Pharmacy and Pharmacology

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Using liposomes to deliver drugs to and through human skin is controversial, as their function varies with type and composition. Thus they may act as drug carriers controlling release of the medicinal agent. Alternatively, they may provide a localized depot in the skin so minimizing systemic effects or can be used for targeting delivery to skin appendages (hair follicles and sweat glands). Liposomes may also enhance transdermal drug delivery, increasing systemic drug concentrations. With such a multiplicity of functions, it is not surprising that mechanisms of liposomal delivery of therapeutic agents to and through the skin are unclear. Accordingly, this article provides an overview of the modes and mechanisms of action of different vesicles as drug delivery vectors in human skin. Our conclusion is that vesicles, depending on the composition and method of preparation, can vary with respect to size, lamellarity, charge, membrane fluidity or elasticity and drug entrapment. This variability allows for multiple functions ranging from local to transdermal effects. Application to dissimilar skins (animal or human) via diverse protocols may reveal different mechanisms of action with possible vesicle skin penetration reaching different depths, from surface assimilation to (rarely) the viable tissue and subsequent systemic absorption.

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Section: Free Drug Mechanism (See Figure 3 At A)contrasting

confidence: 47%

Untitled

2006

Journal of Pharmacy and Pharmacology

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“…Esposito et al (1998) reported that the permeability coefficient of methyl nicotinate is inversely related to the liposome size. Du Plessis et al (1994) showed that the intermediate particle size of 300 nm resulted in both the highest reservoir in the deeper skin layers, as well as the highest drug concentration in the reservoir, confirming that topical drug delivery is influenced by the size of liposomes.…”

Section: Resultsmentioning

confidence: 74%

“…These include diffusion experiments (Du Plessis et al, 1994), visualization by electron microscopy (Hofland et al, 1995;Korting et al, 1995) and micro dialysis (Schnetz and Fartasch, 2001). Micro dialysis and diffusion experiments provide information about the amount and the rate of drug penetration of the model compound, but do not give any information about the physiological effects of the model drug on cells and lipid organization.…”

Section: Introductionmentioning

confidence: 99%

Particle size of liposomes influences dermal delivery of substances into skin

Verma

Blume

et al. 2003

International Journal of Pharmaceutics

545

257

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“…Du Plessis et al (du Plessis et al, 1994) suggested that the intermediate vesicle size of 300 nm gave the best deposition of drug in the deeper skin layers, and the highest drug concentration in the reservoir. During our investigation and method optimization, we therefore aimed for a liposome size distribution between 200-300 nm.…”

Section: Optimization Of the Methodologymentioning

confidence: 99%

Development and optimization of a new processing approach for manufacturing topical liposomes-in-hydrogel drug formulations by dual asymmetric centrifugation

Ingebrigtsen

Škalko‐Basnet

Holsæter

2016

Drug Development and Industrial Pharmacy

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Objectives: The objective of the present study was to utilize dual asymmetric centrifugation (DAC) as a novel processing approach for the production of liposomes-in-hydrogel formulations. Materials and Methods:Lipid films of phosphatidylcholine, with and without chloramphenicol (CAM), were hydrated and homogenized by DAC to produce liposomes in the form of vesicular phospholipid gels with a diameter in the size range of 200-300 nm suitable for drug delivery to the skin. Different homogenization processing parameters were investigated along with the effect of adding propylene glycol (PG) to the formulations prior to homogenization. The produced liposomes were incorporated into a hydrogel made of 2.5 % (v/v) soluble β-1,3/1,6-glucan (SBG) and mixed by DAC to achieve a homogenous liposomes-inhydrogel-formulation suitable for topical application.Results and Discussion: CAM-containing liposomes with a vesicle diameter of 282 ± 30 nm and polydispersity index (PI) of 0.13 ± 0.02 were successfully produced by DAC after 50 minutes centrifugation at 3500 rpm, and homogenously (< 4 % content variation) incorporated into the SBG hydrogel. Addition of PG decreased the necessary centrifugation time to 2 minutes and 55 seconds, producing liposomes of 230 ± 51 nm and PI of 0.25 ± 0.04. All formulations had an entrapment efficiency of approximately 50%. Conclusions:We managed to develop a relatively fast and reproducible new method for the production of liposomes-in-hydrogel formulation by DAC.

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The influence of particle size of liposomes on the deposition of drug into skin

Cited by 175 publications

References 13 publications

Untitled

Untitled

Particle size of liposomes influences dermal delivery of substances into skin

Development and optimization of a new processing approach for manufacturing topical liposomes-in-hydrogel drug formulations by dual asymmetric centrifugation

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