Assessment of the toxicity of lipid nanocapsules and polymer nanoparticles on a neuronal cell model as a first step towards their development for nose-to-brain drug delivery

Nose-to-brain delivery is a promising alternative to deliver therapeutics to the central nervous system, due to the possibility to bypass the blood-brain barrier. Because of their versatility, nanoparticulate delivery systems may offer several advantages for this route. This study investigates the correlation between physicochemical characteristics of two different types of nanomaterials, namely lipid nanocapsules (LNCs) and PLGA nanoparticles (PLGA-NPs), and their behaviour towards SH-SY5Y cells as the neuronal cell model. Physicochemical characterisation and stability studies showed that all the formulations exhibited excellent properties and stability under storage (4 oC) and physiological conditions. Surface hydrophobicity was also assessed wherein PLGA-NPs were found to be generally more hydrophobic compared to LNCs. Cytotoxicity assays towards SH-SY5Y cells suggested that surfactant-related toxicity is more likely to occur in LNCs compared to PLGA-NPs. Cellular uptake was also analysed using flow cytometry and fluorescence microscopy. The results from this study can be used as consideration in developing nanoparticulate delivery system for nose-to-brain delivery

EFFECT OF HONEY CONSUMPTION AFTER PHYSICAL EXERCISES ON ELECTROLYTES AND BLOOD GLUCOSE LEVELS

Honey has been used as food and medicine for thousands of years. The purpose of this study was to determine the effect of honey in restoring the levels of electrolytes and blood glucose after performing physical exercises. The effect of honey consumption on electrolyte and blood glucose levels was examined on12 healthy male subjects, which were divided into 4 groups with three members in each group. Group I was treated as control and provided only 250 ml of mineral water after exercise, while group II was provided 250 ml commercial isotonic beverage, group III  provided honey solution 1 (15 ml honey/250 ml water), and group IV provided honey solution 2 (45 ml honey/250 ml water). The physical exercise performed by the subjects is running on a treadmill at a speed of 5.6 km/h for 40 minutes. Measurements of electrolyte and blood glucose levels were performed 24 hrs before as initial baseline, and these were also measured after the physical exercise as well as after the treatment. Results of the study revealed that honey played a significant role in the restore electrolyte and blood glucose levels in people who have performed physical activities such as exercising and the effect of honey is similar to the commercial isotonic beverage. However, no significant difference (p-value > 0.05) was reported between the honey solution 1 and 2  and other treatment groups in elevating sodium and chloride level

PENGARUH JENIS DAN KONSENTRASI SURFAKTAN TERHADAP KARAKTERISTIK FISIK MIKROEMULSI MINYAK DEDAK PADI

Minyak dedak padi (MDP) memiliki aktivitas antioksidan yang sangat baik sehingga berpotensi untukdikembangkan menjadi bahan aktif sediaan kosmetik. Di dalam penelitian ini, MDP diformulasikan ke dalambentuk mikroemulsi dengan variasi jenis dan konsentrasi surfaktan. MDP yang digunakan pertama-tamadianalisis terlebih dahulu untuk memastikan identitas minyak. Setelah itu, dilakukan pengukuran aktivitasantioksidan, di mana diperoleh nilai IC50 sebesar 239,32 μg/ml terhadap radikal bebas DPPH. Untuk formulasimikroemulsi, campuran surfaktan dan ko-surfaktan yang digunakan adalah Tween 80-Span 80-propilen glikoluntuk tiga formula, dan Cremophor® RH 40-gliserin untuk tiga lainnya. Mikroemulsi MDP dibuat denganmenggunakan metode inversi fase dan setelah itu dilakukan pengamatan terhadap karakteristik fisikmikroemulsi yang dihasilkan, meliputi organoleptis, ukuran globul, viskositas, pH, serta uji pemisahan fase.Secara umum, formulasi yang menggunakan campuran Cremophor® RH 40-gliserin memiliki karakteristik fisikyang lebih baik, Ukuran globul mikroemulsi yang dihasilkan dengan campuran Cremophor® RH 40-gliserinberkisar 21,32 – 24,10 nm dengan indeks polidispersitas <0,3 yang menunjukkan homogenitas ukuran globulyang baik. Hasil uji pemisahan fase juga menunjukkan bahwa formulasi yang menggunakan Cremophor® RH40-gliserin lebih stabil dan tidak mengalami pemisahan fase setelah sentrifugasi

Enhanced skin localization of doxycycline using microparticles and hydrogel: effect of oleic acid as penetration enhancer

One of the disadvantages of gel preparations is the poor ability to penetrate the skin. Herein we developed a sodium carboxymethylcellulose (NaCMC)-based gel containing microparticle of doxycycline hyclate (DOX).  Oleic acid (OA) was added into the gel formulation specifically to increase the penetrability of DOX microparticles. The objective of this work was to determine the effect of varying concentration of OA on the physical characteristics, penetration and retention abilities of DOX. DOX microparticles were initially prepared using PLGA as a matrix and then incorporated into a NaCMC-based gel with various OA concentrations: 0%, 2.5%, 5%, 7.5%, and 10% for F1, F2, F3, F4, and F5, respectively. The gel preparations were evaluated for their organoleptic test, homogeneity, pH measurement, viscosity, spreadability, as well as ex vivo penetration and retention abilities. The physical characteristics tests revealed a homogeneous yellow gel with a distinctive odor and pH values compatible with the pH requirements of human skin. The retention test showed the formulation retained 1236.46 µg of DOX in the skin. Finally, the skin retention of DOX from microparticles loaded gel was significantly higher compared to the free DOX loaded gel, indicating the microparticles can be extremely effective in retaining the DOX in the infected area

Enhanced skin localization of doxycycline using microparticles and hydrogel: effect of oleic acid as penetration enhancer

One of the disadvantages of gel preparations is the poor ability to penetrate the skin. Herein we developed a sodium carboxymethylcellulose (NaCMC)-based gel containing microparticle of doxycycline hyclate (DOX). Oleic acid (OA) was added into the gel formulation specifically to increase the penetrability of DOX microparticles. The objective of this work was to determine the effect of varying concentration of OA on the physical characteristics, penetration and retention abilities of DOX. DOX microparticles were initially prepared using PLGA as a matrix and then incorporated into a NaCMC-based gel with various OA concentrations: 0%, 2.5%, 5%, 7.5%, and 10% for F1, F2, F3, F4, and F5, respectively. The gel preparations were evaluated for their organoleptic test, homogeneity, pH measurement, viscosity, spreadability, as well as ex vivo penetration and retention abilities. The physical characteristics tests revealed a homogeneous yellow gel with a distinctive odor and pH values compatible with the pH requirements of human skin. The retention test showed the formulation retained 1236.46 µg of DOX in the skin. Finally, the skin retention of DOX from microparticles loaded gel was significantly higher compared to the free DOX loaded gel, indicating the microparticles can be extremely effective in retaining the DOX in the infected area

Marine macrolides to tackle antimicrobial resistance of mycobacterium tuberculosis

Tuberculosis has become a major health problem globally. This is worsened by the emergence of resistant strains of Mycobacterium tuberculosis showing ability to evade the effectiveness of the current antimycobacterial therapies. Therefore, the efforts carried out to explore new entities from many sources, including marine, are critical. This review summarizes several marine-derived macrolides that show promising activity against M. tuberculosis. We also provide information regarding the biosynthetic processes of marine macrolides, including the challenges that are usually experienced in this process. As most of the studies reporting the antimycobacterial activities of the listed marine macrolides are based on in vitro studies, the future direction should consider expanding the trials to in vivo and clinical trials. In addition, in silico studies should also be explored for a quick screening on marine macrolides with potent activities against mycobacterial infection. To sum up, macrolides derived from marine organisms might become therapeutical options for tackling antimycobacterial resistance of M. tuberculosis.Directorate General of Higher Education, Ministry of Education, Culture, Research, and Technology, Indonesia | Ref. 020/E5/PG.02.00PT/202