Engineered Dutasteride-Lipid Based Nanoparticle (DST-LNP) System Using Oleic and Stearic Acid for Topical Delivery

Male pattern baldness (MPB) is a common condition that has a negative impact on the psycho-social health of many men. This study aims to engineer an alcohol-free formulation to cater for individuals who may have had allergic reactions to alcohol-based preparations. A lipid-based nanoparticle system composed of stearic and oleic acid (solid and liquid lipid) was used to deliver dutasteride (DST) for topical application. Two compositions, with oleic acid (Formulation A) and without (Formulation B), were compared to analyse the role of oleic acid as a potential active ingredient in addition to DST. DST-loaded LNP were prepared using the emulsification–ultrasonication method. All of the prepared formulations were spherical in shape in the nanometric size range (150–300 nm), with entrapment efficiencies of >75%. X-ray diffractograms revealed that DST exists in an amorphous form within the NLP matrices. The drug release behaviour from both LNP preparations displayed slow release of DST. Permeation studies through pig ear skin demonstrated that DST-LNP with oleic acid produced significantly lower permeation into the dermis compared to the formulation without oleic acid. These results suggest that the proposed formulation presents several characteristics which are novel, indicating its suitability for the dermal delivery of anti-androgenic molecules.

N-Alkylmorpholines: Potent Dermal and Transdermal Skin Permeation Enhancers

Transdermal drug delivery is an attractive non-invasive method offering numerous advantages over the conventional routes of administration. The main obstacle to drug transport is, however, the powerful skin barrier that needs to be modulated, for example, by transdermal permeation enhancers. Unfortunately, there are still only a few enhancers showing optimum properties including low toxicity and reversibility of enhancing effects. For this reason, we investigated a series of new N-alkylmorpholines with various side chains as potential enhancers in an in vitro permeation study, using three model permeants (theophylline, indomethacin, diclofenac). Moreover, electrical impedance, transepidermal water loss, cellular toxicity and infrared spectroscopy measurements were applied to assess the effect of enhancers on skin integrity, reversibility, toxicity and enhancers’ mode of action, respectively. Our results showed a bell-shaped relationship between the enhancing activity and the hydrocarbon chain length of the N-alkylmorpholines, with the most efficient derivatives having 10–14 carbons for both transdermal and dermal delivery. These structures were even more potent than the unsaturated oleyl derivative. The best results were obtained for indomethacin, where particularly the C10-14 derivatives showed significantly stronger effects than the traditional enhancer Azone. Further experiments revealed reversibility in the enhancing effect, acceptable toxicity and a mode of action based predominantly on interactions with stratum corneum lipids.

Invasomes for enhanced delivery through the skin: Evaluation of systems with meet clinical challenges

Background: Portage of therapeutic agents directly to the skin (cutaneous/dermal delivery) is the preferable approach in mitigating and curing a variety of skin manifestations, including itching, eczema, acne, psoriasis keratinization, and skin cancer. Dermal delivery reduces side effects associated with systemic therapy and allows maximum utilization of the available doses. Invasomes are the next generation of liposomes with greater flexibility, elasticity, and permeability through the skin than liposomes and ethosomes. Objective: This review article highlights various aspects of invasomes, including the structure and composition of invasomes, methods of preparation of invasomes, the mechanism involved in better penetration through the skin, key parameters to be considered for effective permeation, therapeutic applications of invasomes as novel drug delivery systems, and future development and challenges. Methods: The authors have reviewed various primary and secondary sources, including PUBMED, SCIENCE DIRECT, INFORMA, and patents.com, to collect information on various aspects of invasomes. Results and Conclusion: Invasomes are novel vesicular drug delivery systems that have been used for dermal delivery of drugs for various therapeutic applications. These novel carriers have great ability, and their properties can be highly modulated by varying their composition and concentration of terpenes. Based on all the research reports gathered, it is well proven that these systems have a much higher potential for delivering drugs for skin manifestations and could expand the opportunities for treating various dermatological issues, increasing day by day.

Treatment of Skin Cancer by Topical Drug Delivery of Nanoparticles: A Review

Nanoparticles offer novel openings for the management of dermal diseases. The skin being a largest organ of the body poses a barrier to all the delivery system including nanoparticles to permeate deep in to the cells or tissues. This barrier was ruptured in case of skin trauma or injury and also in the case of skin cancer. This conditions of the skin allowed the nanoparticles to permeate through the skin for the treatment of cancer. Worldwide research is going in to the formulation and development of the Nano carrier for the dermal delivery through the skin. But the little or negligible technology transfer occur from the R&D to Industry for the treatment of skin cancer using nanoparticles. The main aim of review is to discuss about the basic fundamentals of cancer with relate to dermal delivery of drug through Nanoparticles. The nanotechnologies for dermal delivery of drugs were explained for their effective tool for skin cancer. In this review types of skin cancer with various nanotechnologies were discussed along with pathology of disease and various therapies used. Further we had discussed challenges in developing the nanoparticles for the treatment in the skin cancer therapy. Finally various therapies like Chemotherapies, Immunotherapy, Gene therapy, Nano carriers combined with physical methods and Laser irradiation therapies were summarized.

Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

The present investigation aims at developing models by response surface methodology (FCCCD) followed by the scale-up method in preparing control release microsponge particles loaded with 5- fluorouracil, a drug used to treat actinic keratosis and colon cancer, and producing a new Dermal Delivery System. The polymer-based (ethyl cellulose and eudragit RS 100) microsponge particles were prepared by the w/o/w double emulsification method. The optimized product was formed with the combination of independent variables levels: polymer (600 mg), stirring speed (1198 rpm) and surfactant (2% w/v), yielding responses as yield (~63.6257%), the average size of particles (~151.563 µm), entrapment efficiency (~75.319 %) and drug release in 8hr (~75.75%), with desirability value of 0.737. The products showed similar responses as obtained in scale-up work. FT-IR, DSC and SEM studies confirmed the drug's compatibility with polymers and porous morphology. Finally, gel embedded optimised product showed shear-thinning rheological property, ideal for drug release from the thixotropic gel.