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Dutasteride, used for treating benign prostate hyperplasia (BPH), promotes hair growth. To enhance delivery to the hair follicles and reduce systemic effects, in this study dutasteride has been formulated for topical application, in a nanostructured lipid carrier (NLC) coated with chitosan oligomer-stearic acid (CSO-SA). CSO-SA has been successfully synthesized, as confirmed using 1 H NMR and FTIR. Formulation of dutasteride-loaded nanostructured lipid carriers (DST-NLCs) was optimized using a 2 3 full factorial design. This formulation was coated with different concentrations of stearic acid-chitosan solution. Coating DST-NLCs with 5% SA-CSO increased mean size from 187.6 ± 7.0 nm to 220.1 ± 11.9 nm, and modified surface charge, with zeta potentials being −18.3 ± 0.9 mV and +25.8 ± 1.1 mV for uncoated and coated DST-NLCs respectively. Transmission electron microscopy showed all formulations comprised approximately spherical particles. DST-NLCs, coated and uncoated with CSO-SA, exhibited particle size stability over 60 days, when stored at 4–8 °C. However, NLCs coated with CSO (without conjugation) showed aggregation when stored at 4–8 °C after 30 days. The measured particle size for all formulations stored at 25 °C suggested aggregation, which was greatest for DST-NLCs coated with 10% CSO-SA and 5% CSO. All nanoparticle formulations exhibited rapid release in an in vitro release study, with uncoated NLCs exhibiting the fastest release rate. Using a Franz diffusion cell, no dutasteride permeated through pig ear skin after 48 h, such that it was not detected in the receptor chamber for all samples. The amount of dutasteride in the skin was significantly different ( p < 0.05) for DST-NLCs (6.09 ± 1.09 μg/cm 2 ) without coating and those coated with 5% CSO-SA (2.82 ± 0.40 μg/cm 2 ), 10% CSO-SA (2.70 ± 0.35 μg/cm 2 ) and CSO (2.11 ± 0.64 μg/cm 2) . There was a significant difference ( p < 0.05) in the cytotoxicity (IC 50 ) between dutasteride alone and in the nanoparticles. DST-NLCs coated and uncoated with CSO-SA increased the maximum non-toxic concentration by 20-fold compared to dutasteride alone. These studies indicate that a stearic acid-chitosan conjugate was successfully prepared, and modified the surface charge of DST-NLCs from negative to positive. These stable, less cytotoxic, positively-charged dutasteride-loaded nanostructured lipid carriers, with stearic acid-chitosan oligomer conjugate, are appropriate for topical delivery and have potential for promotion of hair growth. [ABSTRACT FROM AUTHOR]

Virgin coconut oil (VCO) is the finest grade of coconut oil, rich in phenolic content, antioxidant activity and contains medium chain triglycerides (MCTs). In this work formulation, characterisation and penetration of VCO-solid lipid particles (VCO-SLP) have been studied. VCO-SLP were prepared using ultrasonication of molten stearic acid and VCO in an aqueous solution. The electron microscopy imaging revealed that VCO-SLP were solid and spherical in shape. Ultrasonication was performed at several power intensities which resulted in particle sizes of VCO-SLP ranged from 0.608 ± 0.002 μm to 44.265 ± 1.870 μm. The particle size was directly proportional to the applied power intensity of ultrasonication. The zeta potential values of the particles were from −43.2 ± 0.28 mV to −47.5 ± 0.42 mV showing good stability. The cumulative permeation for the smallest sized VCO-SLP (0.608 μm) was 3.83 ± 0.01 μg/cm² whereas for larger carriers it was reduced (3.59 ± 0.02 μg/cm²). It is concluded that SLP have the potential to be exploited as a micro/nano scale cosmeceutical carrying vehicle for improved dermal delivery of VCO. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]