Encapsulation of ascorbyl palmitate in nanostructured lipid carriers (NLC)—Effects of formulation parameters on physicochemical stability

Teeranachaideekul, Veerawat; Müller, Rainer H.; Junyaprasert, Varaporn Buraphacheep

doi:10.1016/j.ijpharm.2007.03.022

Cited by 222 publications

(120 citation statements)

References 25 publications

Supporting

Mentioning

116

Contrasting

Unclassified

Order By: Relevance

“…This should result in a higher loading capacity, encapsulation efficiency and controlled drug release as the drug dissolves in the oil and simultaneously encapsulates in the solid lipid; which should also lead to slower polymorphic transition and lower crystallinity index (higher stability) [20][21][22][23]. The drug of study, ART is photolabile and short-acting, so the major criteria were to find a protective carrier with modified release property as well as good consistency (thickner).…”

Section: Introductionmentioning

confidence: 99%

Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

Nnamani

Hansen

Windbergs

et al. 2014

International Journal of Pharmaceutics

View full text Add to dashboard Cite

NLC topical formulation as an alternative to oral and parenteral (IM) delivery of artemether (ART), a poorly water-soluble drug was designed. A Phospholipon 85G-modified Gelucire 43/01 based NLC formulation containing 75 % Transcutol was chosen from DSC studies and loaded with gradient concentration of ART (100-750 mg). ART-loaded NLCs were stable (-22 to -40 mV), polydispersed (0.4 to 0.7) with d90 size distribution range of 247 to 530 nm without microparticles up to one month of storage. The encapsulation efficiency (EE %) for ART in the NLC was concentration independent as 250 mg of ART loading achieved ~61%. DSC confirmed molecular dispersion of ART due to low matrix crystallinity (0.028 J/g). Ex vivo study showed detectable ART amounts after 20 h which gradually increased over 48 h achieving ~26 % cumulative amount permeated irrespective of the applied dose. This proves that ART permeates excised human epidermis, where the current formulation served as a reservoir to gradually control drug release over an extended period of time. Full thickness skin study therefore may confirm if this is a positive signal to hope for a topical delivery system of ART.

show abstract

Section: Introductionmentioning

confidence: 99%

Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

Nnamani

Hansen

Windbergs

et al. 2014

International Journal of Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…Enhancement of chemical stability after incorporation into lipid nanocarriers was proven for many cosmetic actives, e.g. coenzyme Q10 [164][165][166], ascorbyl palmitate [164,167], tocopherol (vitamin E) [165] and retinol (vitamin A) [168][169][170].…”

Section: Applications Of Nanocarrier Systems In Topical/transdermal Dmentioning

confidence: 99%

Nanocarrier Systems for Transdermal Drug Delivery

Escobar-Chávez¹,

Rodríguez-Cruz²,

Domínguez-Delgado³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

View full text Add to dashboard Cite

is an open discussion, in one hand, the nanotechnologist continue making new and more sophisticated nanocarriers and in the other hand, toxicologist continue evaluating possible damaging effects.Whatever it happens, nanotechnology is the new era and nanomedicine cannot be taking off. New nanocarriers will be created and the entire scientist working in nanomedicine bet for it to be the cure of diseases that in this moment are difficult to deal with [3] The application of preparations to the skin for medical purposes is as old as the history of medicine itself, with references to the use of ointments and salves found in the records of Babylonian and Egyptian medicine. The historical development of permeation research is well described by Hadgraft & Lane [4]. Over time, the skin has become an important route for drug delivery in which topical, regional or systemic effects are desired. Nevertheless, skin constitutes an excellent barrier and presents difficulties for the transdermal delivery of therapeutic agents, since few drugs possess the characteristics required to permeate across the stratum corneum in sufficient quantities to reach a therapeutic concentration in the blood. In order to enhance drug transdermal absorption different methodologies have been investigated developed and patented [5,6]. Improvement in physical permeationenhancement technologies has led to renewed interest in transdermal drug delivery. Some of these novel advanced transdermal permeation enhancement technologies include: iontophoresis, electroporation, ultrasound, microneedles to open up the skin and more recently the use of transdermal nanocarriers [3,[7][8][9][10].A number of excellent reviews that have been published contain detailed discussions concerning many aspects of transdermal nanocarriers [11][12][13][14][15][16][17]. The present chapter shows an updated overview of the use of submicron particles and other nanostructures in the pharmaceutical field, specifically in the area of topical and transdermal drugs. This focus is justified due to the magnitude of the experimental data available with the use of these nanocarriers. The development of submicron particles and other nanostructures in the pharmaceutical and cosmetic fields has been emerged in the last decades for designing best formulations for application through the skin [18][19][20][21]. The skinThe skin is the largest organ of the body [22][23][24], accounting for more than 10% of body mass, and the one that enables the body to interact more intimately with its environment. Essentially, the skin consists of four layers: The SC, that is the outer layer of the skin (nonviable epidermis), and forms the rate-controlling barrier for diffusion for almost all compounds. It is composed of dead flattened, keratin-rich cells, the corneocytes. These dense cells are surrounded by a complex mixture of intercellular lipids, namely, ceramides, free fatty acids, cholesterol, and cholesterol sulphate. Their most important feature is that they are structured as ordered bilayer arrays [25]...

show abstract

“…Since they are made from solid lipids, chemically unstable lipid soluble compounds that are sensitive to oxidation can be successfully encapsulated in the SLNs (8, 10). Several molecules were incorporated into lipid nanoparticles, e.g., ascorbyl palmitate, resveratrol, retinol and retinyl palmitate, vitamin E and vitamin E acetate (8,(11)(12)(13)(14). It has been shown that systemic uptake of active substances (e.g., isotretinoin) through skins could be avoided and SLN could increase the accumulative uptake of the active material in the skin (15).…”

mentioning

confidence: 99%

“…It supports ATP generation during aerobic cellular respiration in the electron transport chain in the mitochondria and inhibits cell membrane peroxidation in reduced form (6,7). However, it is very difficult to prepare a formulation that helps Q10 delivery to deeper layers of the skin due to the low aqueous solubility of Q10 (log P >10) and due to the barrier function of stratum corneum (8).…”

mentioning

confidence: 99%

“…SLNs have many advantages, especially for dermal applications such as occlusion, modulation of drug release and penetration into the skin (9). Since they are made from solid lipids, chemically unstable lipid soluble compounds that are sensitive to oxidation can be successfully encapsulated in the SLNs (8,10). Several molecules were incorporated into lipid nanoparticles, e.g., ascorbyl palmitate, resveratrol, retinol and retinyl palmitate, vitamin E and vitamin E acetate (8,(11)(12)(13)(14).…”

mentioning

confidence: 99%

See 1 more Smart Citation

Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

Korkm¹,

Gökçe²,

Özer³

2013

Acta Pharmaceutica

View full text Add to dashboard Cite

Skin is the protective organ of the body with an area around 2 m 2 . The hazardous potential of toxins, pathogens and UV radiation are avoided by the protection that skin supplies (1). UV radiation is the main source of energy that initiates reactive oxygen species (ROS). Formation of ROS leads to oxidative damage in DNA, proteins and lipids. The skin has an enzymatic (superoxide dismutase, catalase, and glutathione peroxidase) and non-enzymatic (antioxidant) protection mechanism against these damages; however, excess ROS production overcomes this protection and causes several diseases such as cancer (2, 3). Hence, effective delivery of an antioxidant into skin in required levels is an important challenge. There are two main steps limiting the effective delivery antioxidants, oxidation of the active substance and carrying the active substance to the viable epidermis.Antioxidants are defined as substances that, when present in a low concentration compared to that of oxidizable substrates, significantly delay or inhibit oxidation of that substance (4). In general, antioxidants act by the chain breaking reaction, by reducing the concentration of reactive oxygen species, by scavenging initiating radicals and by chelating transition metal catalysts (5). Coenzyme Q10 (Q10) is the only lipid soluble endogenous antioxidant. It supports ATP generation during aerobic cellular respiration in the electron transport chain in the mitochondria and inhibits cell membrane peroxidation in reduced form (6, 7). However, it is very difficult to prepare a formulation that helps Q10 delivery to deeper layers of the skin due to the low aqueous solubility of Q10 (log P >10) and due to the barrier function of stratum corneum (8).In the second half of the nineties there was an increasing interest in investigating solid lipid nanoparticles (SLNs) for dermal application. SLNs have many advantages, especially for dermal applications such as occlusion, modulation of drug release and penetration into the skin (9). Since they are made from solid lipids, chemically unstable lipid soluble compounds that are sensitive to oxidation can be successfully encapsulated in the SLNs (8, 10). Several molecules were incorporated into lipid nanoparticles, e.g., ascorbyl palmitate, resveratrol, retinol and retinyl palmitate, vitamin E and vitamin E acetate (8,(11)(12)(13)(14). It has been shown that systemic uptake of active substances (e.g., isotretinoin) through skins could be avoided and SLN could increase the accumulative uptake of the active material in the skin (15). SLNs are produced as liquid dispersions and their incorporation into hydrogels or emulsions helps enhance the retention time in the applied area and patient compliance (16,17).Hydrogels are generally formed from carbomers that have the ability to absorb water, get hydrated and swell by neutralization with a base. Carbomers have been mainly used in liquid or semi-solid pharmaceutical formulations in order to modify their flow characteristics (17,18).The aim of this work was to carry an effic...

show abstract

Encapsulation of ascorbyl palmitate in nanostructured lipid carriers (NLC)—Effects of formulation parameters on physicochemical stability

Cited by 222 publications

References 25 publications

Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

Nanocarrier Systems for Transdermal Drug Delivery

Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

Contact Info

Product

Resources

About