Degradation Pathways of Therapeutic Peptides in Aqueous Solutions and Strategies to Improve Stability

A number of hormones, enzymes, antitumor agents, antibiotics and neurotransmitters are peptides. Nowadays, peptides are used as therapeutic agents against diverse disease areas such as neurological, endocrinological and hematological disorders. Therapeutic peptides pose a number of challenges for pharmaceutical scientists regarding their formulation and delivery. The sensitivity of many peptides to enzymatic breakdown and their poor ability to pass absorbing membranes typically results in a poor bioavailability following non-parenteral administration. Therefore, parenteral administration is the most commonly used route for systemic delivery of peptide drugs. However, therapeutic peptides are often unstable in aqueous solution limiting their shelf life. The lack of physical and chemical stability may lead to significant degradation during processing and storage of the (aqueous) formulations. Although a dry powder for reconstitution may overcome the lack of physical and chemical stability, from an economic point of view aqueous liquid formulations are preferred. In this presentation the main peptide stability problems in solution will be introduced following known strategies to inhibit peptide degradation, including recent research on improving peptide stability in liquid formulations. In conclusion, the most useful stabilization approaches are optimizing the pH and the type of buffer. Co-solvency, air exclusion, and viscosity enhancement can also be useful to reduce the degradation rate

Process Optimization for Green Synthesis of Silver Nanoparticles Using Indonesian Medicinal Plant Extracts

Silver nanoparticles (AgNPs) are an interesting metal nanoparticle that can be incorporated into pharmaceutical products, including for diabetic foot ulcers as an antimicrobial agent. Green synthesis of AgNPs using plant extracts has been drawing much attention as it is simple, eco-friendly, stable, and cost-effective. This present study was performed to evaluate the potential of three Indonesian medicinal plant extracts, namely Phyllanthus niruri (PN), Orthosiphon stamineus (OS), and Curcuma longa (CL), as reducing and capping agents in the green synthesis of AgNPs, and to optimize their concentrations. Based on the yields and characteristics of the formed nanoparticles, which were analyzed using a UV-Vis spectrophotometer, particle size analyzer, scanning electron microscope, and X-ray diffractometer, Phyllanthus niruri extract at a concentration of 0.5% was concluded as the best extract in the green synthesis of AgNPs. It is thereby a prospective reducing and capping agent for further scale-up studies

EFFECT OF MILLING PROCESS ON PHYSICAL CHARACTERISTICS OF FENOFIBRATE

Particle size is ones of the most important characteristic of active drug substance that affects solubility and bioavailability. Fenofibrate, as a class II drug based on biopharmaceutical classification system, which has poor aqueous solubility has been chosen to be drug model of particle size reduction.. Fenofibrate was mixed with mannitol as stabilizer with the ratio 1:9 in physical mixture form. The size reduction was conducted by a ball mills, with the milling rate of 100, 200 and 300 rpm, respectively. Characterization of the solid dispersion was analyzed by organoleptic and instrumental method. The instrumental tools used were Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) which showed that there was no changes happen in fenofibrate molecule during milling process. Scanning Electron Microscope results showed that fenofibrate-mannitol was produce non-spherical forms. Milling rate improvement produce smaller size of particle with rough morphology that decrease the flow properties. Based on the solubility test and reflected in UV/Vis spectra, it showed that particle size reduction with 200 rpm milling rate determined 3 times higher of aborsbance value compared with pure fenofibrate

EFEKTIVITAS PENGAWET PADA PRODUK LOKAL EYELINER WATERPROOFTERHADAP PERTUMBUHAN Pseudomonas aeruginosadan Candida albicans YANG DIJUAL DI PASAR BLAURAN KOTA SURABAYA

Abstract – The purpose of this study was to test the effectiveness of preservatives on waterproof eyeliner sold in Pasar Blauran Surabaya. The method used in this research is Total Plate Numbers (ALT) using Nutrient Agar (NA) media for Pseudomonas aeruginosa and Saboraud Dextrose Agar with addition of antibiotic (SDAa) for Candida albicans to obtain a 5,6 x 108CFU / ml suspension for Pseudomonas aeruginosa and 2.0 x 107 CFU / ml for Candida albicans. Then the suspension was added to the sample, then observed the growth of bacterial colony and yeast on the 2nd and 7th day. The result obtained is no growth of Pseudomonas aeruginosa and Candida albicans on day 2 and 7, so preservative in the sample can be said to be effective in inhibiting the growth of bacteria and yeasts

EFEKTIVITAS PENGAWET PADA PRODUK LOKAL EYELINER WATERPROOFTERHADAP PERTUMBUHAN Pseudomonas aeruginosadan Candida albicans YANG DIJUAL DI PASAR BLAURAN KOTA SURABAYA

Abstract – The purpose of this study was to test the effectiveness of preservatives on waterproof eyeliner sold in Pasar Blauran Surabaya. The method used in this research is Total Plate Numbers (ALT) using Nutrient Agar (NA) media for Pseudomonas aeruginosa and Saboraud Dextrose Agar with addition of antibiotic (SDAa) for Candida albicans to obtain a 5,6 x 108CFU / ml suspension for Pseudomonas aeruginosa and 2.0 x 107 CFU / ml for Candida albicans. Then the suspension was added to the sample, then observed the growth of bacterial colony and yeast on the 2nd and 7th day. The result obtained is no growth of Pseudomonas aeruginosa and Candida albicans on day 2 and 7, so preservative in the sample can be said to be effective in inhibiting the growth of bacteria and yeasts

Aktivitas Penghambat Reseptor-β Adrenergik Ekstrak Air Kulit Batang Taya (Nauclea subdita (Korth) Steud) Pada Tikus Wistar Jantan

Beta-adrenergic receptor blockers (β-blockers) are an appropriate treatment for patients with hypertension who have concomitant ischemic hearat disease, heart failure, obstructive cardiomyopathy, aortic dissection or certain cardiac arrhythmias. Taya (Nauclea subdita (Korth) Steud) is a local natural potential of Kalimantan that is empirically believed to have antihypertensive activities. This study aims to determine the activity of β-adrenergic receptor inhibitors of stem bark water extract in male wistar rats. Tests were carried out on male Wistar rats by the Non Invasive Blood Pressure method using the CODA® tool. Test animals were divided into 5 groups: normal group, induction group (Epinephrine 1.2 µg/kgBW), 100 mg/kgBW extract group, 200 mg/kgBW extract group, and 4,5 mg/kgBW atenolol group. The induction group showed an increase in systolic blood pressure, diastolic blood pressure, and heart rate that were significantly different from the normal group, the 100 mg/kgBW extract group, the 200 mg/kgBW extract extract group, and the 4.5 mg/kgBW atenolol group (p<0,05). The 100 mg/kgBW extract group was not significantly different from systolic blood pressure, diastolic blood pressure, and heart rate with the normal group, the 200 mg/kgBW extract group, and the 4.5 mg/kgBW atenolol group (p> 0.05). The results of this study showed that taya bark water extracts 100 mg/kgbw had inhibitory activity of β-adrenergic receptors in male wistar rats.Beta-adrenergic receptor blocker (β-blocker) merupakan salah satu antihipertensi yang tepat digunakaan untuk pasien hipertensi yang disertai penyakit jantung iskemik, gagal jantung, kardiomiopati obstruktif, diseksi aorta, atau aritmia jantung tertentu. Tanaman taya (Nauclea subdita (Korth) Steud) merupakan potensi lokal alam Kalimantan yang secara empiris diyakini memiliki aktivitas sebagai antihipertensi. Penelitian ini bertujuan untuk mengetahui aktivitas inhibisi ekstrak air kulit batang taya pada reseptor-β adrenergik . Pengujian menggunakan tikus wistar jantan dengan metode Non Invasive Blood Pressure (CODA®). Hewan uji dibagi menjadi 5 kelompok yaitu kelompok normal, kelompok induksi (Epinefrin 1,2 µg/kgBB), kelompok ekstrak 100 mg/kgBB, kelompok ekstrak 200 mg/kgBB, dan kelompok atenolol 4,5 mg/kgBB. Kelompok induksi menunjukkan kenaikan tekanan darah sistolik, tekanan darah diastolik, dan detak jantung yang berbeda signifikan dengan kelompok normal, kelompok ekstrak 100 mg/kgBB, kelompok ekstrak 200 mg/kgBB, dan kelompok atenolol 4,5 mg/kgBB (p<0,05). Kelompok ekstrak 100 mg/kgBB berbeda tidak signifikan tekanan darah sistolik, tekanan darah diastolik, dan detak jantung dengan kelompok normal, kelompok ekstrak 200 mg/kgBB, dan kelompok atenolol 4,5 mg/kgBB (p>0,05). Hasil penelitian ini menunjukkan ekstrak air kulit batang taya dosis 100 mg/kgbbmemiliki aktivitas menghambat reseptor-β adrenergik pada tikus wistar jantan

EFEKTIVITAS PENGAWET PADA PRODUK LOKAL EYELINER WATERPROOFTERHADAP PERTUMBUHAN Pseudomonas aeruginosadan Candida albicans YANG DIJUAL DI PASAR BLAURAN KOTA SURABAYA

Abstract – The purpose of this study was to test the effectiveness of preservatives on waterproof eyeliner sold in Pasar Blauran Surabaya. The method used in this research is Total Plate Numbers (ALT) using Nutrient Agar (NA) media for Pseudomonas aeruginosa and Saboraud Dextrose Agar with addition of antibiotic (SDAa) for Candida albicans to obtain a 5,6 x 108CFU / ml suspension for Pseudomonas aeruginosa and 2.0 x 107 CFU / ml for Candida albicans. Then the suspension was added to the sample, then observed the growth of bacterial colony and yeast on the 2nd and 7th day. The result obtained is no growth of Pseudomonas aeruginosa and Candida albicans on day 2 and 7, so preservative in the sample can be said to be effective in inhibiting the growth of bacteria and yeasts

Thermostability and free radical scavenging activity of Annona muricata (L.) leaf extract in antiaging cream

Annona muricata is an Indonesian medicinal plant commonly used as an anticancer agent. The finding of its strong antioxidant activity leads to the development of cosmetic products, particularly as antiaging cream. Formulation may influence thermostability and free radical scavenging activity of A.muricata leaf extract. The purpose of this study was to investigate the thermostability and free radical scavenging activity of A.muricata leaf extract incorporated in Gattefosse Skin Cashmere cream. Accelerated stability study utilizing climatic chamber at a temperature of 40ºC 2ºC and relative humidity of 75% 5% for 20 days of storage was used to evaluate thermostability. 1,1- diphenyl-2-picrylhydrazil (DPPH) using spectrophotometer was used for free radical scavenging activity test. The result from physical properties including appearance of antiaging cream, pH, viscosity and rheological properties of each formula showed that all of the formulas were stable at a temperature of 40ºC 2ºC and relative humidity of 75% 5% for 20 days. Free radical scavenging activity using DPPH showed high antioxidant activities from the A.muricata leaf extract in the Gattefosse Skin Cashmere cream. We concluded that A. muricata leaf extract could be developed into natural antiaging cosmetic product