Advanced Pharmaceutical Technology & Research

Physicochemical properties of Arenga pinnata Merr. endosperm and its antidiabetic activity for nutraceutical application Juliati Br Tarigan, Diana A Barus, Aminah Dalimunthe, Sabarmin Perangin-Angin, Trung T Nguyen Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):1-5 This study aims to provide information on physicochemical properties of Arenga pinnata endosperm (APE) and its antidiabetic activity for utilization in the food and pharmaceutical industries. The antidiabetic effect of APE was studied through an observational experiment on the blood glucose level of rats. The physicochemical properties of APE were determined using a texturometer, X-ray powder diffraction, Brookfield viscometer, scanning electron microscopy, Fourier-transform infrared spectroscopy, and light microscope. The APE was categorized based on its texture into three groups. The crystal structure of APE is microspore and amorf while the hydrogel has a non-Newtonian property and is stable at 50°C. The viscosity index was increased in the increasing temperature with the order of high viscosity of APE being 1, 2, and 3. The hydrogel shape of APE 1 and 3 was lameral in the concentration of 1.25%. For antidiabetic study, the findings demonstrated that the APE could reduce the blood glucose level. The APE powders 1 and 2 with the respective weight of 50 and 200 mg have significant effects on reducing rat blood glucose level compared to the diabetic rats. Based on these properties, APE could potentially be used as a natural antidiabetic food without having any side effect and in the pharmaceutical industry for some purposes.

The purity identification and radiolabeling of α-mangostin with technetium-99m Muchtaridi Muchtaridi, Luthfi Utami Setyawati, Risda Rahmi Islamiaty, Kevin Reinard Lie, Wiwit Nurhidayah Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):6-12 Alpha-mangostin (AM) is a natural compound that has the greatest activity in breast cancer. Radiolabeling AM with technetium-99 m (Tc-99m) has a function as breast cancer radiotracer. This study is aimed to identify the purity of Tc-99m-labeled AM. The identification method was conducted by a validated radio-high-performance liquid chromatography (HPLC) to confirm the chemical purity of the compound when the thin layer of chromatography and paper chromatography were used to find out the radiochemical purity (RCP). The validated radio-HPLC method obtained was C18 column with methanol:water (90:10) as the mobile phase and ultraviolet (243 nm) tandem radioactive detector (Gabi Star). The result showed that the RCP was 70.6% ± 2.87%. The analytical method met the validation criteria according to ICH Q2 (R1); thus, it could be applied in the identification. Unfortunately, the99mTc-AM identification using radio-HPLC showed that the expected complex was not yet formed perfectly because of chemical impurities.

Design and optimization of topical terbinafine hydrochloride nanosponges: Application of full factorial design, in vitro and in vivo evaluation Reham I Amer, Ghada H El-Osaily, Sameh S Gad Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):13-19 Terbinafine hydrochloride (THCl) has a broad-spectrum antifungal activity. THCl has oral bioavailability 40%, which increases dosing frequency of the drug, thus leads to some systemic side effects. Sustained release THCl nanosponges hydrogel was fabricated to deliver the drug topically. Pure THCl (drug), polyvinyl alcohol (emulsifier), and ethyl cellulose (EC, polymer to produce nanosponges) were used. THCl nanosponges were produced successfully by the emulsion solvent evaporation method. Based on a 32 full factorial design, different THCl: EC ratios and stirring rates were used as independent variables. The optimized formula selected based on the particle size and entrapment efficiency % (EE) was formulated as topical hydrogel. All formulations were found in the nanosize range except F7and F9. EE was ranged from 33.05% to 90.10%. THCl nanosponges hydrogel released more than 90% of drug after 8 h and showed the highest in vivo skin deposition and antifungal activity. The increase in drug: EC ratio was observed to increase EE and the particle size while higher stirring rate resulted in finer emulsion globules and significant reduction in EE. The drug release profile was slow from dosage form when it was incorporated in entrapped form as nanosponges rather than unentrapped one. The nanosponges hydrogel succeeded to sustain THCl release over 8 h. It showed the highest antifungal activity and skin deposition. THCl nanosponges hydrogel represents an enhanced therapeutic approach for the topical treatment of fungal infection.

The cytotoxicity test of calcium hydroxide, propolis, and calcium hydroxide-propolis combination in human pulp fibroblast Ira Widjiastuti, Mieke Kusuma Dewi, Edhi Arief Prasetyo, Nirawati Pribadi, Mochamad Moedjiono Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):20-24 Calcium hydroxide (Ca(OH)2) is the gold standard material used for pulp-capping but still has a high failure rate. Thus, an alternative material is needed, one of which is propolis. The combination of Ca(OH)2propolis is expected to have better quality and to be biocompatible. The aim of this study is to investigate the viability of human pulp fibroblast after the administration of Ca(OH)2, propolis, and its combination. Human pulp fibroblast culture derived from premolar teeth of 16-year-old patients, were divided into seven groups: Group 1 (10 μg Ca(OH)2); Group 2 (10 μg propolis); Group 3 (15 μg propolis); Group 4 (20 μg propolis); Group 5 (Ca(OH)2-propolis 1:1); Group 6 (Ca(OH)2-propolis 1:1.5); and Group 7 (calcium hydroxide-propolis 1:2). They were placed in a 96 wells plate and put into incubator for 24 h. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test was conducted to calculate the viability of human pulp fibroblasts. The data were analyzed statistically using Kolmogorov–Smirnov, Levene's test, one-way analysis of variance, and Tukey-honestly significant difference (P < 0.05). The number of living human pulp fibroblast after the administration of Ca(OH)2and propolis combination is greater than the application of Ca(OH)2or propolis with significant different between groups (P < 0.05). The viability of human pulp fibroblasts after the administration of Ca(OH)2-propolis combination is greater than that of the application of Ca(OH)2and propolis alone.

Characterization, antioxidant, antimycobacterial, antimicrobial effcts of Moroccan rosemary essential oil, and its synergistic antimicrobial potential with carvacrol Marwa Chraibi, Abdellah Farah, Oumaima Elamin, Houssaini Mohammed Iraqui, Kawtar Fikri Benbrahim Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):25-29 Thanks to their promising properties, essential oils (EOs) have strong potential to remedy several problems such as microorganisms acquired resistance to antimicrobial agents and chemical antioxidants toxicity. Firstly, this work was conducted to determine chemical composition, antioxydant activity, then antibacterial, antifungal, antimycobacterial properties of Rosmarinus officinalis EO. Secondly, EOs combined antimicrobial effect with carvacrol was assessed. Chemical EO analysis was performed using Gas chromatography/mass spectrometer. 1,1-diphenyl-2-picrylhydrazyl test was used to evaluate in vitro antioxidant rosemary oil effect. The antimicrobial activity against seven bacteria, two fungi, and two mycobacterial strains was screened using the broth microdilution method. Thereafter, the checkerboard essay was used to evaluate the antibacterial effect of this EO and Carvacrol. Chemical EO analysis revealed 1,8-cineole (33.88%), camphor (14.66%), and α-pinene (12.76%) as main constituents. The obtained IC50 value (2.77 mg/mL) showed rosemary EO's radical scavenging power. Moreover, all tested microorganisms showed an important sensitivity to this EO (MIC values: 0.007%–1% (v/v)). Furthermore, results highlighted synergistic and partial synergistic interaction for tested products. The studied EO has both antimicrobial and antioxidant potentials. Combined application showed a remarkable synergistic antibacterial potentiation that can be used as an alternative in pharmaceutical and food processing sectors.

Antihypercholesterolemic and antiatherosclerotic potencies of Pandanus tectorius fruits via increasing scavenger receptor-B1 genes expression and inhibition of 3-hydroxy-3-methylglutaryl coenzyme: A reductase activity Yosie Andriani, Gul-e-Saba Chaudhry, Efriyana Oksal, Inten Pangestika, Nadia Madiha Ramli, Habsah Mohamad, Rina Elvia, Hermansyah Amir, Effendy AWM, Yeong Yik Sung, Tengku Sifzizul Tengku Muhammad Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):30-35 Atherosclerosis is a leading cause of death worldwide. The adverse side effects of currently available drugs urge to find more effective and safe remedial agents. Alternative candidates from natural resources are of great consequence in the emerging of new drugs. Pandanus tectorius (Pandanaceae) was traditionally used in Ayurvedic medicine to cure certain diseases. Thus, the current study conducted to elucidate the potency of P. tectorius fruit as antiatherosclerosis and antihypercholesterolemia agents through the regulation of high density lipoprotein (HDL) receptor (scavenger receptor [SR]-B1) gene expression and 3-hydroxy-3-methylglutaryl coenzyme A reductase reductase (HMGCR) in vitro, respectively. The P. tectorius fruit was noncytotoxic against the HepG2 cell line confirmed by 3-(4,5-dimethylthiazol-2-yl) 2,5-diphenyl tetrazolium bromide assay. The P. tectorius fruit successfully upregulates the SR-B1 gene expression and downregulate the HMGCR. Moreover, an in vivo study showed that P. tectorius has good activity on the upregulation of HDL and subsequently downregulation of total cholesterol level. Moreover, P. tectorius fruit did not show any increase in toxicity biomarkers serum glutamic oxaloacetic transaminase and serum glutamate pyruvate transaminase in vivo. These results found that P. tectorius fruits have potency as the preventive agent for hypercholesterolemia and atherosclerosis via SR-B1 and HMGCR mechanisms of action.

Polymeric worm-like nanomicellar system for accelerated wound healing Aarti Singh, Adeeba Shakeel, Dakshi Kochhar, Sampathkumar Jeevanandham, Satyendra Kumar Rajput, Monalisa Mukherjee Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):36-43 Self-assembly is an unparalleled step in designing macromolecular analogs of nature's simple amphiphiles. Tailoring hydrogel systems – a material with ample potential for wound healing applications – to simultaneously alleviate infection and prompt wound closure is vastly appealing. The poly (DEAEMA-co-AAc) (PDEA) is examined with a cutaneous excisional wound model alterations in wound size, and histological assessments revealed a higher wound healing rate, including dermis proliferation, re-epithelialization, reduced scar formation, and anti-inflammatory properties. Moreover, a mechanism for the formation of spherical and worm-like micelles (WLMs) is delineated using a suite of characterizations. The excellent porosity and ability to absorb exudates impart the PDEA with reliable wound healing. Altogether, this system demonstrates exceptional promise as an infection-mitigating, cell-stimulating, homeostasis-maintaining dressing for accelerated wound healing. The aim and objective of this study is to understand the mechanism of self-assembly in synthesized WLMs from PDEA and their application in wound healing.

Antidiabetic effect of Drymaria cordata leaf against streptozotocin–nicotinamide-induced diabetic albino rats Susmita Patra, Sanjib Bhattacharya, Asis Bala, Pallab Kanti Haldar Journal of Advanced Pharmaceutical Technology & Research 2020 11(1):44-52 Drymaria cordata (Caryophyllaceae), commonly known as Abhijalo in Sikkimese-Tibetan, is a creeping herb grown in tropical and subtropical regions of the world. It is used by ethnic groups of Sikkim, North-East India, for the treatment of various diseases including diabetes. This study aimed to investigate the antidiabetic effect of methanol extract from D. cordata leaf (DCME) in streptozotocin (STZ) and nicotinamide (NA)-induced type 2 diabetes in rats. Diabetic Wistar albino rats were treated with DCME at 200 mg/kg and 400 mg/kg orally for 28 days. Metformin (150 mg/kg b.w.) was used as a reference drug. Fasting blood glucose (FBG) level; serum biochemical parameters; and liver, kidney, and antioxidant parameters were estimated, and pancreatic histopathology was performed after 28 days of treatment. Administration of DCME to STZ-NA-induced diabetic rats at 200 mg/kg and 400 mg/kg orally for 28 days exhibited statistically significant (P < 0.05) and dose-dependent reduction of FBG, glycosylated hemoglobin, serum lipid, and hepatorenal antioxidative parameters in DCME-treated groups when compared to those of diabetic controls. Histopathological studies of pancreas in DCME-treated rats showed improvement in β-cell density compared to diabetic group. The results demonstrate the significant antidiabetic potential of D. cordata leaf in albino rats plausibly by reducing oxidative stress and serum lipids levels, justifying the folkloric use of this plant in the treatment of diabetes.