Development and in vitro evaluation of a liposomal vaginal delivery system for acyclovir

Pavelić, Željka; Škalko‐Basnet, Nataša; Filipović-Grčić, Jelena; Martinac, Anita; Jalšenjak, Ivan

doi:10.1016/j.jconrel.2005.03.032

Cited by 134 publications

(65 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…When we began establishing the DAC-procedure we aimed to investigate the possibility of integrating the polyol dilution method as the first step of liposome production, inspired by the work of Kikuchi and colleagues (Kikuchi et al, 1994) and others (Pavelić et al, 1999, Pavelić et al, 2005, but in combination with DAC. The polyol dilution method makes it possible to avoid the use of harmful organic solvents in the production process, replacing them with PG to dissolve both CAM and PC.…”

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

Self Cite

View full text Add to dashboard Cite

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.

show abstract

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

Self Cite

View full text Add to dashboard Cite

show abstract

“…To follow the release of diclofenac sodium from the liposomes-in-vehicle formulations, we applied a so-called agarose method that has been shown to be very useful in evaluating drug release from liposomal vaginal gels 14,16,23 . The porosity of the agarose matrix permitted both intact liposomes and released (free) drug to diffuse through the matrix into the receptor 10 solution, and the amount of drug released from the vehicle was determined spectrophotometrically before and after the addition of methanol to the supernatant over the agarose matrix 16 .…”

Section: Liposomes-in-vehicle Formulationsmentioning

confidence: 99%

“…The release of the drug from the liposomes incorporated into different vehicles was determined by the method originally introduced by Pesckha et al 25 and adapted for liposomal hydrogels 14,16,23 . Briefly, samples of the liposomes-in-vehicle formulations (3 g) were placed in glass vials and separated from 5 mL of receptor solution (distilled water) by a 2% (w/w) agarose layer, which permitted diffusion of both the released drug and intact liposomes from liposomes-in-vehicles (donor compartment).…”

Section: 5mentioning

confidence: 99%

“…Vehicle composition has been shown to influence the release properties of the incorporated drug and the penetration ability across/into the skin and may also improve the skin condition 3,4,33 . To examine the effect of the vehicle on the release of liposomally entrapped diclofenac sodium, different types of liposomes were incorporated into the following vehicles: the hydrogel, the cream base (O/W emulsion) and DMS base.To follow the release of diclofenac sodium from the liposomes-in-vehicle formulations, we applied a so-called agarose method that has been shown to be very useful in evaluating drug release from liposomal vaginal gels 14,16,23 . The porosity of the agarose matrix permitted both intact liposomes and released (free) drug to diffuse through the matrix into the receptor 10 solution, and the amount of drug released from the vehicle was determined spectrophotometrically before and after the addition of methanol to the supernatant over the agarose matrix 16 .…”

mentioning

confidence: 99%

See 1 more Smart Citation

Elastic liposomes-in-vehicle formulations destined for skin therapy: the synergy between type of liposomes and vehicle

Palac

Hurler

Škalko‐Basnet

et al. 2014

Drug Development and Industrial Pharmacy

Self Cite

View full text Add to dashboard Cite

Objective: The present study is focused on optimization of elastic liposomes-in-vehicle formulations in respect to drug release and formulation properties. By combining penetration potential of elastic liposomes containing high ratio of entrapped drug and physicochemical properties of vehicles, both affecting the release and texture properties, optimal formulation could be achieved. Materials and methods:Deformable, propylene glycol-containing or conventional liposomes with hydrophilic model drug (diclofenac sodium) were incorporated into the following vehicles appropriate for skin application: a hydrogel, a cream base and derma membrane structure base cream (DMS base). Each formulation was assessed for in vitro drug release and mechanical properties. Results and discussion:The composition and type of both liposomes and the vehicle affected the rate and amount of the released drug. The cream base exhibited the slowest release, followed by the hydrogel and DMS base. Similar release profiles were achieved with both types of elastic vesicles (deformable and propylene glycol liposomes); the slowest release was observed for conventional liposomes, regardless of the vehicle used. The drug release profiles from different liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. All of the liposomes were found to be compatible with the hydrogel preserving its original textures, whereas a significant decrease in all texture parameters was observed for liposomes-in-DMS base, regardless of liposome type. Conclusion:Propylene glycol liposomes-in-hydrogel is considered as the optimal formulation for improving skin delivery of hydrophilic drug. Further investigations involving in vivo animal studies are necessary to confirm its applicability in skin therapy. INTRODUCTIONEffective (trans)dermal drug delivery depends on both the selection of an appropriate drug and the properties of the delivery system (vehicle). Vehicles exert pronounced effects on the epidermis, affecting hydration, lubrication, drying, skin smoothness, occlusion and protection.In addition, the physicochemical properties of vehicles influence the pharmacokinetic properties of the incorporated drug by controlling its release from the vehicle and affecting penetration through the stratum corneum, permeation through the layers of skin and absorption into the blood. Preparation and characterization of liposomesDeformable, propylene glycol and conventional liposomes were prepared by the film 6The mean diameters, size distributions (polydispersity) and zeta potentials of the liposomes were determined by photon correlation spectroscopy (Zetasizer 3000HS, MalvernInstruments, Malvern, UK) 20,21 . Membrane elasticity of extruded liposomes was evaluated by home-made device at an external pressure of 5 bar using 100-nm membranes. Detailed procedure with equation for calculation of the deformability degree (E) has been previously described in details 14,19 . Separation of the unentrapped drug was performed usin...

show abstract

“…In the development of nanotherapeutics, nanotechnology tools are used to improve drug solubility (eg, micelles 7 and nanocrystals 8 ), to guide drugs to the desired location of action with increased precision (ie, drug targeting 9,10 ), to control the drug's release (eg, nanoparticles 11 and liposomes 12 ), and/or to enhance the transport across biological barriers (eg, micelles 13 and nanoparticles 14 ). The main goal is to improve drug bioavailability, pharmacokinetics, efficacy, and safety to promote the treatment of diseases which currently cannot be achieved with conventional dosage forms.…”

Section: Introductionmentioning

confidence: 99%

Nanotherapeutics in the EU: an overview on current state and future directions

Hafner¹,

Lovrić²,

Lakoš³

et al. 2014

IJN

113

View full text Add to dashboard Cite

The application of nanotechnology in areas of drug delivery and therapy (ie, nanotherapeutics) is envisioned to have a great impact on public health. The ability of nanotherapeutics to provide targeted drug delivery, improve drug solubility, extend drug half-life, improve a drug’s therapeutic index, and reduce a drug’s immunogenicity has resulted in the potential to revolutionize the treatment of many diseases. In this paper, we review the liposome-, nanocrystal-, virosome-, polymer therapeutic-, nanoemulsion-, and nanoparticle-based approaches to nanotherapeutics, which represent the most successful and commercialized categories within the field of nanomedicine. We discuss the regulatory pathway and initiatives endeavoring to ensure the safe and timely clinical translation of emerging nanotherapeutics and realization of health care benefits. Emerging trends are expected to confirm that this nano-concept can exert a macro-impact on patient benefits, treatment options, and the EU economy.

show abstract

Development and in vitro evaluation of a liposomal vaginal delivery system for acyclovir

Cited by 134 publications

References 24 publications

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

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

Elastic liposomes-in-vehicle formulations destined for skin therapy: the synergy between type of liposomes and vehicle

Nanotherapeutics in the EU: an overview on current state and future directions

Contact Info

Product

Resources

About