Cutaneous bioavailability in hairless rats of tretinoin in liposomes or gel

Masini, V.; Bonté, Frédéric; Meybeck, Alain; Wépierre, J.

doi:10.1002/jps.2600820104

Cited by 85 publications

(27 citation statements)

References 4 publications

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“…The study on liposomes for targeting drugs into the pilosebaceous units has suggested that liposomes are potent drug delivery systems for treating hair follicle-associated disorders, such as acne (Kumar & Katare, 2004;Yang et al, 2009). Incorporation of tretinoin in liposomes to overcome its problems has been studied by several researchers (Foong et al, 1990;Masini et al,1993;Patel et al, 2000;Brisaert et al, 2001;Sinico et al, 2005). It was previously found that liposomes can increase tretinoin concentration in the epidermis and dermis when compared to conventional cream or gel (Manconi et al, 2003).…”

Section: Introductionmentioning

confidence: 99%

Tretinoin-loaded liposomal formulations: from lab to comparative clinical study in acne patients

et al. 2015

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Topical tretinoin is the most commonly used retinoid for acne. However, its irritative potential on the applied area and the barrier properties of the stratum corneum limit its use. The objective of the present study was to formulate tretinoin liposomal gel to obtain a formula with lower skin irritation potential and greater clinical effect. A statistical 2 4 factorial design was adopted. Sixteen formulae prepared and were properly evaluated. A candidate formula (F13G) prepared with 0.025% tretinoin, phospholipid-cholesterol-dicetylphosphate (9:1:0.01) and incorporated in 1% carbopol gel was selected for skin irritation test. Clinical study was conducted on acne patients and compared to marketed product. All liposomes formulations were spherical in shape. The addition of cholesterol in the film hydration method significantly decreased the vesicle size, and increased the percentage of incorporation efficiency at (p50.05). The presence of dicetylphosphate significantly increased drug release but did not affect the percentage of incorporation efficiency and vesicle size. The results of the clinical study in acne patients revealed that F13G showed significantly higher efficacy when compared to marketed product (p50.05).

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Section: Introductionmentioning

confidence: 99%

Tretinoin-loaded liposomal formulations: from lab to comparative clinical study in acne patients

et al. 2015

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“…Photodegradation render the drug ineffective and also causes allergy due to degradation products (7,8). In order to overcome the limitations of present topical therapy, carrier approach such as liposomes (9), niosomes (10) and solid lipid nanoparticles (11) for effective delivery of isotretinoin have been reported. It has been found that, topically applied liposomes increase the residence time of isotretinoin in stratum corneum and reduces its systemic absorption (9).…”

Section: Introductionmentioning

confidence: 99%

“…In order to overcome the limitations of present topical therapy, carrier approach such as liposomes (9), niosomes (10) and solid lipid nanoparticles (11) for effective delivery of isotretinoin have been reported. It has been found that, topically applied liposomes increase the residence time of isotretinoin in stratum corneum and reduces its systemic absorption (9). Although, many authors have proposed the use of tretinoin liposomal formulations, but no work has been carried out on tretinoin elastic liposomal formulations.…”

Section: Introductionmentioning

confidence: 99%

Drug-Cyclodextrin-Vesicles Dual Carrier Approach for Skin Targeting of Anti-acne Agent

2010

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Abstract. In the present study attempt was made for preparation of isotretinoin-hydroxypropyl β cyclodextrin (HP-β-CD) inclusion complex and encapsulate this complex in elastic liposomes to study the effect of dual carrier approach on skin targeting of isotretinoin. The isotretinoin HP-β-CD complex was prepared by freeze-drying method and characterized by IR spectroscopy. The drug and drug-CD complex loaded elastic liposomal formulation were prepared and characterized in vitro, ex-vivo and in vivo for shape, size, entrapment efficiency, no. of vesicles per cubic mm, in vitro skin permeation and deposition study, photodegradation and skin toxicity assay. The transdermal flux for different vesicular formulations was observed between 10.5±0.5 to 13.9±1.6 μg/cm 2 /h. This is about 15-21 folds higher than that obtained from drug solution (0.7 ±0.1 μg/cm 2 /h) and 4-5 folds higher than obtained with drug-CD complex solution (2.7±0.1 μg/cm 2 /h). The amount of drug deposit was found to increase significantly (p<0.05) by cyclodextrin complexation (30.1±0.1 μg). The encapsulation of this complex in elastic liposomal formulation further increases its skin deposition (262.2 ±21 μg). The results of skin irritation study using Draize test also showed the significant reduction in skin irritation potential of isotretinoin elastic liposomal formulation in comparison to free drug. The results of the present study demonstrated that isotretinoin elastic liposomal formulation possesses great potential for skin targeting, prolonging drug release, reduction of photodegradation, reducing skin irritation and improving topical delivery of isotretinoin.

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“…deeper stratum corneum, epidermis and dermis [10]. Thus, liposomes can be used as transdermal drug delivery systems [8,11].…”

Section: Introductionmentioning

confidence: 99%

Biodegradable Liposomes for Acyclovir-Gold Nanoparticles as an Efficient Carrierfor Enhanced Topical Delivery

Salem

Tamam

Lotayef

2017

Int J Pharm Pharm Sci

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Objective: Gold nanoparticles and nanoliposomes are effective new technology in delivering the bioactive agents and enhancing their performance by increasing the bioavailability. The goal of the present study was the formulation of liposome for the use as a carrier for nanogold conjugated with acyclovir (ACV), an antiviral drug, to enhance ACV delivery. Methods:The gold nanoparticles were used as a capping agent for ACV and sodium citrate was used as reducing agent for the gold. Transmission electron microscopy was used for characterization and to study the morphological and structural properties of drug-metallic nanostructures. Nanoliposomes were formulated using different molar ratios of a positive charge inducer (stearyl amine) or a negative charge inducer (diacetyl phosphate), lecithin, cholesterol and Span 60.Results: Gold nanoparticles with a particle size of 10-20 nm were formed. This small size of the formed particles has a clear effect in reducing the gold nanoparticles toxicity and enhancing the cellular uptake. The amount of sodium citrate used in this preparation influences the size of the gold nanoparticle. The present study employed 1% trisodium citrate that contains a carboxylic group and this carboxylic group works as a reducing and capping agent to synthesize ACV-gold nanoparticles conjugate. Liposomal formula F6 had the highest entrapment efficiency approaching 42%, the low particle size of 160 nm, and zeta potential of 43.5 mV. Conclusion:It is evident from the study that the liposomes can be used as a carrier of ACV conjugated with gold nanoparticles. This new strategy could be used successfully in the treatment of viral infection.

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Cutaneous bioavailability in hairless rats of tretinoin in liposomes or gel

Cited by 85 publications

References 4 publications

Tretinoin-loaded liposomal formulations: from lab to comparative clinical study in acne patients

Tretinoin-loaded liposomal formulations: from lab to comparative clinical study in acne patients

Drug-Cyclodextrin-Vesicles Dual Carrier Approach for Skin Targeting of Anti-acne Agent

Biodegradable Liposomes for Acyclovir-Gold Nanoparticles as an Efficient Carrierfor Enhanced Topical Delivery

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