Review articleNanostructured lipid carriers: A potential use for skin drug delivery systems
Introduction
The oral route is the most important and conventional method of drug administration. Unfortunately, oral drug delivery systems have many significant limitations, such as drug degradation in the gastrointestinal track (by enzymes, pH), pre-systemic metabolism or toxic side effects. One of the methods which could overcome problems associated with the oral route is transdermal drug delivery (TDD) [1,2]. Application of drugs in the liquid, semisolid or solid form to treat skin diseases has been used since the beginning of humanity. Later, the next goal was to use skin for transdermal drug delivery to provide the systemic therapy. The first transdermal therapeutic system was developed in 1981 in the form of a patch with scopolamine (Transdermal Scop®) for the treatment of motion sickness. Today, there is a great variety of transdermal products for drugs such as nitroglycerin, clonidine, fentanyl, nicotine, oestradiol, testosterone or diclofenac [3,4].
TDD has obvious advantages over other routes of delivery. It can improve compliance, especially for patients who do not tolerate oral dosage forms, including people who are unconscious or those with swallowing problems. It also allows for pain-free and safe administration of drugs, in addition to reducing the frequency of their application. Another advantage of TDD is assurance of more consistent serum drug levels, elimination of hepatic first-pass metabolism, avoidance of drug degradation in the gastrointestinal tract and reduction of side effects (e.g. gastrointestinal upsets) [1,5,6]. The main disadvantage of transdermal drug delivery concerns low permeability of skin, which limits drug penetration. Furthermore, some drugs and excipients used in transdermal formulations can cause skin irritation (erythema, itching, edema) or allergic reaction [7,8].
Section snippets
Problems with dermal and transdermal drug administration
Skin is the largest multilayered organ of the body, with a surface area of 1.7 - 2.0 m2. Microscopically, skin consists of three layers: the epidermis (outer layer), the dermis (middle layer) and subcutaneous tissue (inner layer). The epidermis is a stratified and squamous membrane composed of several cell layers and it can be divided into the non-viable epidermis (stratum corneum, SC) and the viable epidermis. The SC consists of keratin-filled corneocytes that are anchored in a lipophilic
Lipid-based formulations as effective dermal vehicles for drugs
Nanotechnology is a modern and rapidly evolving trend in dermal and transdermal drug delivery which includes several forms of nanocarriers such as liposomes, nanoemulsions, nanocrystals, polymeric nanoparticles, lipid nanocarriers and dendrimers. Lipid nanocarriers show essential advantages over conventional drug forms and they are formulated with biodegradable, non-toxic and non-irritant lipids. The small size (from 40 to 800 nm) of lipid nanocarriers allows to adhere them to the lipid film of
Conclusions
Applying drugs to the skin has become an evolutive method for treatment of local and systemic diseases. Replacing conventional dermatological drug forms (ointments, gels) with nanolipids has the main aim of obtaining small particle size and increased penetration of drugs through the skin. The modern form of lipid nanocarriers are nanostructured lipid carriers (NLC). NLC are used particularly for drugs that dissolve poorly in water. The process of obtaining an effective form of NLC requires
Financial support
This article was supported by Medical University of Bialystok grant (No. N/ST/ZB/18/001/2215).
Conflict of interest
The authors declare no conflicts of interest.
References (149)
- et al.
Breaching the skin barrier through temperature modulations
J Control Release
(2015) - et al.
Potential of combined ultrasound and microneedles for enhanced transdermal drug permeation: a review
Eur J Pharm Biopharm
(2015) - et al.
Breakthrough discoveries in drug delivery technologies: the next 30 years
J Control Release
(2014) - et al.
Chemical penetration enhancers in stratum corneum – relations between molecular effects and barrier function
J Control Release
(2016) - et al.
From nanoemulsions to nanostructured lipid carriers: a relevant development in dermal delivery of drugs and cosmetics
J Drug Deliv Sci Tech
(2016) - et al.
Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products
Int J Pharm
(2009) - et al.
Solid lipid nanoparticles as attractive drug vehicles: composition, properties and therapeutic strategies
Mat Sci Eng C
(2016) - et al.
Nanostructured lipid matrices for improved microencapsulation of drugs
Int J Pharm
(2002) - et al.
Nanostructured lipid carriers: promising drug delivery systems for future clinics
Nanomed – Nanotechnol
(2016) - et al.
Characterization and evaluation of nanostructured lipid carrier as a vehicle for oral delivery of etoposide
Eur J Pharm Sci
(2011)
Effects of lipophilic emulsifiers on the oral administration of lovastatin from nanostructured lipid carriers: physicochemical characterization and pharmacokinetics
Eur J Pharm Biopharm
Formulation, characterization and pulmonary deposition of nebulized celecoxib encapsulated nanostructured lipid carriers
J Control Release
Preparation, macrophages targeting delivery and anti-inflammatory study of pentapeptide grafted nanostructured lipid carriers
Int J Pharm
Development of an itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application
Int J Pharm
Montelukast-loaded nanostructured lipid carriers. Part I: oral bioavailability improvement
Eur J Pharm Biopharm
Mucoadhesive effect of thiolated PEG stearate and its modified NLC for ocular drug delivery
J Control Release
Thiolated nanostructured lipid carriers as a potential ocular drug delivery system for cyclosporine A: improving in vivo ocular distribution
Int J Pharm
Novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan for efficient ocular delivery
J Pharm Sci
Improved and safe transcorneal delivery of flurbiprofen by NLC and NLC-based hydrogels
J Pharm Sci
A controlled-release ocular delivery system for ibuprofen based on nanostructured lipid carriers
Int J Pharm
Preparation and in vitro-in vivo evaluation of ofloxacin loaded ophthalmic nano structured lipid carriers modified with chitosan oligosaccharide lactate for the treatment of bacterial keratitis
Eur J Pharm Sci
Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application
Int J Pharm
Development, characterization, and in vitro and in vivo evaluation of benzocaine- and lidocaine-loaded nanostructrured lipid carriers
J Pharm Sci
Ultra-small lipid nanoparticles promote the penetration of coenzyme Q10 in skin cells and counteract oxidative stress
Eur J Pharm Biopharm
A new topical formulation for psoriasis: development of methotrexate-loaded nanostructured lipid carriers
Int J Pharm
Development of a quercetin-loaded nanostructured lipid carrier formulation for topical delivery
Int J Pharm
Progesterone lipid nanoparticles: scaling up and in vivo human study
Eur J Pharm Biopharm
Characterization and biocompatibility evaluation of cutaneous formulations containing lipid nanoparticles
Int J Pharm
Nanostructured lipid carriers for transdermal delivery of acid labile lansoprazole
Eur J Pharm Biopharm
Passive and active strategies for transdermal delivery using co-encapsulating nanostructured lipid carriers: in vitro vs. In vivo studies
Eur J Pharm Biopharm
Development of nanostructured lipid carriers for the encapsulation and controlled release of vitamin D3
Food Chem
Optimizing SLN and NLC by 2(2) full factorial design: effect of homogenization technique
Mater Sci Eng C
Nitrogen doping in atomic layer deposition grown titanium dioxide films by using ammonium hydroxide
Thin Solid Films
Transdermal drug delivery: innovative pharmaceutical developments based on disruption of the barrier properties of the stratum corneum
Pharmaceutics
Dermatology
Food and drug administration: approved drug products with therapeutic equivalence evaluations
Transdermal drug delivery
Nat Biotech
Tocopheryl phosphate mixture (TPM) as a novel lipid-based transdermal drug delivery carrier: formulation and evaluation
Drug Deliv Transl Res
Device-assisted transdermal drug delivery
Adv Drug Deliv Rev
A review on transdermal drug delivery
IJAPBC
Transdermal drug delivery: an overview
Int J Res Dev Pharm L Sci
The structure and function of skin
Transdermal drug delivery in vitro using diffusion cells
Curr Med Chem
Perspective on transdermal drug delivery
J Chem Pharm Res
Transdermal drug delivery system: a review
IJPSR
Permeation pathway of macromolecules and nanospheres through skin
Biol Pharm Bull
Skin permeabilization for transdermal drug delivery: recent advances and future prospects
Expert Opin Drug Deliv
Application of Nanotechnology in Drug Delivery
Transdermal drug delivery: the inherent challenges and technological advancements
Asian J Pharm Sci
Recent advances in gel technologies for topical and transdermal drug delivery
Drug Dev Ind Pharm
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