Please confirm you are human (Sign Up for free to never see this)
← Back to Search
Development Of Pilosebaceous Unit-Targeted Drug Products
G. W. Lu, K. Warner, Fangjing Wang
Published 2014 · Computer Science
Save to my Library
Download PDFAnalyze on Scholarcy
The present chapter outlines the rationale, advances, methods, and product development processes of pilosebaceous unit (PSU)-targeted topical drug products. Since the anatomic structure of the pilosebaceous unit provides a possible pathway for targeted drug delivery into hair follicles and sebaceous glands, significant progress has been made in the area of PSU-targeted drug delivery over past 20 years. Discovery of new chemical entities (NCEs) targeting the PSU is being explored in part because the physical/chemical properties of NCEs are not ameniable for transepidermal penetration. As a formulation approach, micro-/nanoparticulate systems, micro-/nanovesicular systems, and excipients enhancing follicular delivery have been widely investigated for PSU-targeted drug delivery. Several dermal products with these micro-/nanostructures are commercialized for possible enhancement of follicular delivery. Product development process pathways are illustrated using a stage-dependent approach. Considering the complexity, rate of success, cost, and time, product development strategy for NCEs are significantly different from that for an existing drug molecule. The methods for the characterization, testing, quality control of dermal products, and in vitro and in vivo models for nonclinical development are also summarized in the present chapter. Despite substantial advances in the science and technology, it is still challenging to develop commercial prescription (Rx) products based on PSU-targeted mechanisms.
This paper references
Determination of percutaneous absorption by in vitro techniques
R. Bronaugh (1999)
RU 58841-myristate--prodrug development for topical treatment of acne and androgenetic alopecia.
Universitätsklinikum Münster (2005)
Relative influence of ethanol and propylene glycol cosolvents on deposition of minoxidil into the skin.
S. Tata (1994)
Nanocarriers for Effective Topical Delivery of Anti-Infectives
P. Prabhu (2012)
Development of an in vitro Modified Skin Absorption Test for the Investigation of the Follicular Penetration Pathway of Caffeine
S. Trauer (2010)
Lipid nanoparticles as novel delivery systems for cosmetics and dermal pharmaceuticals
C. Puglia (2012)
Development of a new solid lipid nanoparticle formulation containing retinoic acid for topical treatment of acne
G. A. Castro (2007)
Diazepam-Loaded Solid Lipid Nanoparticles: Design and Characterization
G. Abdelbary (2009)
Lipid nanocapsules for dermal application: a comparative study of lipid-based versus polymer-based nanocarriers.
Mona M A Abdel-Mottaleb (2011)
Investigation of Follicular and Non-follicular Pathways for Polyarginine and Oleic Acid-Modified Nanoparticles
Pinaki R. Desai (2012)
Adapalene microemulsion for transfollicular drug delivery.
Gaurav Bhatia (2013)
Enhancement of follicular delivery of finasteride by liposomes and niosomes 1. In vitro permeation and in vivo deposition studies using hamster flank and ear models.
M. Tabbakhian (2006)
Evaluation of the permeability of hair growing ingredient encapsulated PLGA nanospheres to hair follicles and their hair growing effects.
H. Tsujimoto (2007)
Skin permeating nanogel for the cutaneous co-delivery of two anti-inflammatory drugs.
P. Shah (2012)
Retinoids in the treatment of skin aging: an overview of clinical efficacy and safety
S. Mukherjee (2006)
The hamster flank organ model: is it relevant to man?
T. J. Franz (1989)
Topical delivery enhancement with multilamellar liposomes into pilosebaceous units: I. In vitro evaluation using fluorescent techniques with the hamster ear model.
L. Lieb (1992)
Adv. Drug Delivery Rev.
F. Welt (1997)
Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies
K. Bhaskar (2009)
Nanoparticle-based targeting of vaccine compounds to skin antigen-presenting cells by hair follicles and their transport in mice.
Brice Mahé (2009)
Prediction of Percutaneous Penetration: Methods, Measurements, Modelling
L. K. Pershing (1991)
40 nm, but not 750 or 1,500 nm, nanoparticles enter epidermal CD1a+ cells after transcutaneous application on human skin.
A. Vogt (2006)
A new method to improve penetration depth of dyes into the follicular duct: potential application for laser hair removal.
C. Sumian (1999)
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery.
L. Mitchell (2010)
Topical liposome delivery of molecules to hair follicles in mice.
L. Li (1997)
Formulation of Nano and Micro PLGA Particles of the Model Peptide Insulin: Preparation, Characterization, Stability and Deposition in Human Skin
F. Wang (2008)
Penetration and storage of particles in human skin: perspectives and safety aspects.
J. Lademann (2011)
Microneedle/nanoencapsulation-mediated transdermal delivery: Mechanistic insights
Y. Gomaa (2014)
The use of SLN and NLC as topical particulate carriers for imidazole antifungal agents.
E. Souto (2006)
The DEBR rat model for alopecia areata.
R. Oliver (1991)
Nanoparticles in dermatology
Dimitrios Papakostas (2011)
In vitro cytotoxicity assays of solid lipid nanoparticles in epithelial and dermal cells
D. M. Ridolfi (2011)
Deposition of salicylic acid into hamster sebaceous glands
M. R. Motwani (2004)
Designer nanoparticles: incorporating size, shape and triggered release into nanoscale drug carriers
M. Caldorera-Moore (2010)
Nanoparticles--an efficient carrier for drug delivery into the hair follicles.
J. Lademann (2007)
Enhancement of Topical Delivery from Biodegradable Nanoparticles
Rocx00EDo Alvarez-Romx00E1n (2004)
Stability Testing of New Drug Substances and Products
S. Niazi (2016)
Investigations on skin permeation of hyaluronic acid based nanoemulsion as transdermal carrier
M. Kong (2011)
The stumptailed macaque as a model for baldness: effects of minoxidil
H. Uno (1986)
Nanostructured lipid carriers (NLC) in cosmetic dermal products.
R. Mueller (2007)
Mechanism of percutaneous absorption. II. Transient diffusion and the relative importance of various routes of skin penetration.
R. Scheuplein (1967)
Mechanism of percutaneous absorption. 3. The effect of temperature on the transport of non-electrolytes across the skin.
I. Blank (1967)
Dermatological And Transdermal Formulations
K. Walters (2002)
Atlas of Hair and Nails
M. Hordinsky (1999)
Encapsulation of ascorbyl palmitate in nanostructured lipid carriers (NLC)--effects of formulation parameters on physicochemical stability.
Veerawat Teeranachaideekul (2007)
On the mechanism of sebaceous secretion
D. Downing (2004)
Enhanced delivery of drugs into and across the skin by ethosomal carriers
E. Touitou (2000)
Follicular and percutaneous penetration pathways of topically applied minoxidil foam.
U. Blume-Peytavi (2010)
Drug Delivery to the Skin From Sub-micron Polymeric Particle Formulations: Influence of Particle Size and Polymer Hydrophobicity
X. Wu (2009)
Essentials of human anatomy
R. T. Woodburne (1969)
Hamster ear model for sebaceous glands.
G. Plewig (1977)
Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
Z. Urbán-Morlán (2010)
Selective follicular targeting by modification of the particle sizes.
A. Patzelt (2011)
Cosmetics and the skin
F. Wells (1964)
Drug delivery routes in skin: a novel approach.
B. Barry (2002)
Topical delivery of liposomally encapsulated gamma-interferon.
J. du Plessis (1992)
Transfollicular drug delivery--is it a reality?
V. Meidan (2005)
Morphometric studies of the hamster flank organ: an improved model to evaluate pharmacologic effects on sebaceous glands.
A. Weissmann (1984)
Site‐specific methylene blue delivery to pilosebaceous structures using highly porous nylon microspheres: An experimental evaluation
S. Mordon (2003)
Site-Specific Drug Delivery to Pilosebaceous Structures Using Polymeric Microspheres
A. Rolland (2004)
Investigation of drug partition property in artificial sebum.
Satyanarayana Valiveti (2008)
Changes in sebum secretion and the sebaceous gland.
D. Downing (1986)
Are commercially available nanoparticles safe when applied to the skin?
T. A. Robertson (2010)
Investigation of Polylactic Acid (PLA) Nanoparticles as Drug Delivery Systems for Local Dermatotherapy
F. Rancan (2009)
Penetration of nanoparticles into human skin.
X. W. Liang (2013)
Enhanced transfollicular delivery of adriamycin with a liposome and iontophoresis
I. Han (2004)
Chitosan-solid lipid nanoparticles as carriers for topical delivery of tretinoin.
D. M. Ridolfi (2012)
Patented herbal formulations and their therapeutic applications.
Mohamed Musthaba (2010)
Skin Permeation of Small-Molecule Drugs, Macromolecules, and Nanoparticles Mediated by a Fractional Carbon Dioxide Laser: The Role of Hair Follicles
Woan-Ruoh Lee (2012)
Polymorphic behaviour of Compritol®888 ATO as bulk lipid and as SLN and NLC
E. Souto (2006)
Histology of normal skin.
C. Urmacher (1990)
Design and In Vitro Evaluation of Finasteride-Loaded Liquid Crystalline Nanoparticles for Topical Delivery
Thiagarajan Madheswaran (2012)
Targeted delivery of a poorly water-soluble compound to hair follicles using polymeric nanoparticle suspensions.
M. Morgen (2011)
Role of the appendageal pathway in the percutaneous absorption of pyridostigmine bromide in various vehicles
F. Bamba (2010)
Anatomical variation in the amount and composition of human skin surface lipid.
R. Greene (1970)
Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN) dispersions
C. Freitas (1998)
Drug delivery into the skin by degradable particles.
W. Mak (2011)
Relative uptake of minoxidil into appendages and stratum corneum and permeation through human skin in vitro.
J. Grice (2010)
Time and depth resolved visualisation of the diffusion of a lipophilic dye into the hair follicle of fresh unfixed human scalp skin.
Y. Grams (2004)
Preparation and in vitro evaluation of topical formulations based on polystyrene-poly-2-hydroxyl methacrylate nanoparticles.
X. Wu (2009)
A facile construction strategy of stable lipid nanoparticles for drug delivery using a hydrogel-thickened microemulsion system.
Huabing Chen (2010)
Preparation and characterization of solid lipid nanoparticles (SLN) made of cacao butter and curdlan.
Byung-Do Kim (2005)
Novel micelle formulations to increase cutaneous bioavailability of azole antifungals.
Y. G. Bachhav (2011)
Formulation parameters determining the physicochemical characteristics of solid lipid nanoparticles loaded with all-trans retinoic acid.
Soo-Jeong Lim (2002)
Penetration profile of microspheres in follicular targeting of terminal hair follicles.
R. Toll (2004)
Visualization and quantitation of iontophoretic pathways using confocal microscopy.
N. G. Turner (1998)
How to improve R&D productivity: the pharmaceutical industry's grand challenge
S. Paul (2010)
Topical FK506: a potent immunotherapy for alopecia areata? Studies using the Dundee experimental bald rat model
K. McElwee (1997)
The structure and function of skin
K. Walters (2002)
Modulation of drug release from nanocarriers loaded with a poorly water soluble drug (flurbiprofen) comprising natural waxes.
D. Baviskar (2012)
The influence of particle size of liposomes on the deposition of drug into skin
J. Plessis (1994)
Formulation and Characterization of Lipid-Coated Tobramycin Particles for Dry Powder Inhalation
G. Pilcer (2006)
Characterization of diazepam submicron emulsion interface: role of oleic acid.
M. Y. Levy (1994)
Squalene-Containing Nanostructured Lipid Carriers Promote Percutaneous Absorption and Hair Follicle Targeting of Diphencyprone for Treating Alopecia Areata
Yin-Ku Lin (2012)
Nanoparticles and microparticles for skin drug delivery.
T. Prow (2011)
Skin distribution and pharmaceutical aspects of adapalene gel.
J. Allec (1997)
Differential stripping demonstrates a significant reduction of the hair follicle reservoir in vitro compared to in vivo.
A. Patzelt (2008)
Nanocarrier-based topical drug delivery for the treatment of skin diseases
M. Gupta (2012)
Combination of Microneedles with PLGA Nanoparticles as a Potential Strategy for Topical Drug Delivery
W. Zhang (2011)
Preparation, characterization and physico-chemical properties of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC): their benefits as colloidal drug carrier systems.
Melike Üner (2006)
Polymeric nanoparticles-based topical delivery systems for the treatment of dermatological diseases.
Zheng Zhang (2013)
Transdermal delivery of mixnoxidil with block copolymer nanoparticles.
Jongwon Shim (2004)
Methods for quantifying intrafollicular drug delivery: a critical appraisal
V. Meidan (2010)
Non-clinical Safety Studies for the Conduct of Human Clinical Trials for Pharmaceuticals: ICH M3 and M3(R2)
P. Sjöberg (2013)
Differential stripping: determination of the amount of topically applied substances penetrated into the hair follicles.
A. Teichmann (2005)
Transdermal iontophoretic delivery of enoxacin from various liposome-encapsulated formulations.
J. Fang (1999)
Non-invasive delivery of nanoparticles to hair follicles: a perspective for transcutaneous immunization.
A. Mittal (2013)
Comparison of stratum corneum penetration and localization of a lipophilic model drug applied in an o/w microemulsion and an amphiphilic cream.
A. Teichmann (2007)
Production of Solid Lipid Nanoparticles-Drug Loading and Release Mechanism
R. Parhi (2010)
Comparison of artificial sebum with human and hamster sebum samples.
G. W. Lu (2009)
Diffusion properties of model compounds in artificial sebum.
Satyanarayana Valiveti (2007)
The C3H/HeJ mouse and DEBR rat models for alopecia areata: review of preclinical drug screening approaches and results
J. Sun (2008)
Correlation between long-term stability of solid lipid nanoparticles (SLN) and crystallinity of the lipid phase.
C. Freitas (1999)
Targeted transfollicular delivery of artocarpin extract from Artocarpus incisus by means of microparticles.
Tasana Pitaksuteepong (2007)
Skin penetration and distribution of polymeric nanoparticles.
R. Alvarez-Román (2004)
Penetration of Titanium Dioxide Microparticles in a Sunscreen Formulation into the Horny Layer and the Follicular Orifice
J. Lademann (1999)
In‐vitro permeation of drugs into porcine hair follicles: is it quantitatively equivalent to permeation into human hair follicles?
Yakov Frum (2008)
Topical transport of hydrophilic compounds using water-in-oil nanoemulsions.
H. Wu (2001)
Transfollicular Drug Delivery
A. C. Lauer (2004)
Skin hydration and possible shunt route penetration in controlled estradiol delivery from ultradeformable and standard liposomes
Gamal M. M. El Maghraby (2001)
This paper is referenced by
Hair Coloration by Gene Regulation: Fact or Fiction?
T. Matamá (2015)
Histological assessment of follicular delivery of flutamide by solid lipid nanoparticles: potential tool for the treatment of androgenic alopecia
H. Hamishehkar (2016)