DEVELOPMENT OF LIQUISOLID FORMULATION FOR IMPROVED SUSTAINED RELEASE OF PROPRANOLOL HYDROCHLORIDE

Objective: The aim of this study was to develop a liquisolid formulation of propranolol hydrochloride to obtain an improved sustained release profile by varying the ratio of liquid vehicles. Methods: In this study, propranolol hydrochloride (PPH) was dispersed in the combination of propylene glycol and polysorbate 80, as the liquid vehicles, with different ratios. Eudragit® RL and Aerosil® were used as carrier and coating materials, respectively, to produce a dry and free-flowing powder. In addition, HPMC was used to amplify the retardation effect. The prepared formulations were evaluated for its physicochemical properties, including loss on drying, flow rate, angle of repose calculation, drug content analysis, FT-IR spectroscopy, as well as dissolution studies. The obtained dissolution profiles were subsequently fitted to the mathematical model in order to determine the drug kinetics. Results: The results show that all formulations performed dry and free-flowing granules containing PPH in the range of 7-9%. Furthermore, all the prepared formulations were able to sustain the drug release for a total of 8 h in two different dissolution media, namely simulated gastric fluid and simulated intestinal fluid. F4 containing propylene glycol and polysorbate 80 (1:2) possessed the lowest drug release rate. It was also obtained that F1 and F3 followed first-order kinetics while F2, F4, and F5 complied with the Higuchi model. Conclusion: Overall, there was no difference in all the dissolution profiles based on the calculation of the difference and similarities factor

Formulasi Ekstrak Buah Mengkudu (Morinda citrifolia) dalam Bentuk Sediaan Transdermal Liposome Cream

Indonesia is a country rich in herbs. One of them is Noni (Morinda citrifolia). Noni fruit has good benefits for the body such as natural antioxidants and several other benefits. The use of noni fruit as herbal medicine is often used but the way make was still very inadequate to get the optimum effect on the plant. One effort that can be done is to make it a cream preparation liposomes that are used topically. Aims of this research was formulation of Transdermal liposome cream from noni fruit extract. The result showed that the total phenolic content of the extract of noni fruit was as much as 180 µg GAE/g ekstrak. The result of the evaluation of transdermal liposome cream preparation obtained both formulas have viscosity of 9,000 cps and 38.000 cps respectively, have uniform vesicle shape, high adsorption efficiency of 95% and 96,67%, but in formula 2 pH obtained did not fulfill the criteria of topical preparation, while formula 1 fulfilled the criterion that is 6,5. From these results it can be concluded that the noni fruit extract can be prepared in the form of transdermal cream preparations which have good physical characteristics achieved by formula 1

Investigation of Antituberculosis from Medicinal Plant of Community Ethnic in South Sulawesi

Background: Tuberculosis is one of the transmitted diseases that has been claimed as one of the most serious health problems worldwide resulting in death, as reported in WHO in Global Tuberculosis Report 2014. It has been predicted that 9 million people suffer from tuberculosis disease and 1.5 - 2 million deaths occur by this disease. Objective: The aim of this research is to know the species of plant used as anti-hematemesis medicine that has the activity of antituberculosis and antituberculosis-MDR and then investigate the phytochemistry characteristics of the compound from every parts of the plant extract that show the activity of antituberculosis and antituberculosis-MDR which is indicated by the value of Minimum Inhibitory Concentration (MIC) of the extracts. Method: The extraction method used in this research was the maceration method. The antituberculosis activity test was investigated using MODS and LJ media methods. The isolation of the active compound was carried out using Bioassay Guided Fractionation and then the compound characteristics were identified using spectroscopy data. Results: The results showed that extracts from Talas (Collocasia esculenta tuber) and Kariango (Acorus calamus rhizome) plants were active against M. tuberculosis. The FTIR spectroscopy data showed that three isolates obtained from Talas plants contained aliphatic OH and C-O and CH groups. The MIC values of kariango and Talas extracts using the MODS method were 45 mg/ml and 40 mg/ml, respectively. Conclusion: Talas (Collocasia esculenta) tuber and Kariango rhizome ethanolic extract have a potency for antituberculosis and anti-MDR tuberculosis drugs

DEVELOPMENT OF METRONIDAZOLE MICROSPONGE INCORPORATED INTO CARBOMER-BASED VAGINAL GEL

Bacterial vaginosis (BV) is a vaginal infection caused by excessive bacterial growth, thus disrupting the natural balance of bacteria inside the vagina. Metronidazole becomes a drug of choice and a widely prescribed drug for the treatment of BV. However, when applied topically, metronidazole has a low vaginal residence time because of the natural washing mechanism of the vagina. This study aimed to improve the retention time of metronidazole inside the vagina and control its release profile. This study was prepared 4 formulas of gel for metronidazole microsponges with some concentration ratio of carbomer and triethanolamine. The evaluations carried out to test the efficacy of the developed formulation included organoleptic, pH measurement, spreadability, viscosity, mucoadhesive properties, permeation test using Franz diffusion cell and retention test. The results showed that the gel appearance was white, odourless and homogenous. The characteristics of all prepared gel for pH, viscosity, spreadability, and mucoadhesive ability were appropriate to the required standard for vaginal delivery. The permeation and retention test showed that F3 with the carbomer and triethanolamine concentration of 1.25%: 1.75% was able to retain and controlled the drug release locally in the vaginal mucosa. This study provides an alternative strategy in drug formulation for the treatment of BV

Systemic delivery of tenofovir alafenamide using dissolving and implantable microneedle patches

The human immunodeficiency virus (HIV) remains a global health concern, with 37.7 million people currently living with the infection and 1.5 million new cases every year. Current antiretroviral (ARV) therapies are administered through the oral route daily, often in lifelong treatments, leading to pill fatigue and poor treatment adherence. Therefore, the development of novel formulations for the administration ARV drugs using alternative routes is actively sought out. In this sense, microneedle array patches (MAPs) offer a unique user-centric platform that can be painlessly self-applied to the skin and deliver drugs to the systemic circulation. In this work, dissolving and implantable MAPs loaded with the tenofovir alafenamide (TAF) were developed with the aim of releasing the drug systemically. Both MAPs were sufficiently strong to pierce excised neonatal full-thickness porcine skin and form drug depots. In vitro release experiments performed in dialysis membrane models, demonstrated a relatively fast delivery of the drug in all cases. Franz cells experiments revealed that dissolving and implantable MAPs deposited 47.87 ​± ​16.33 ​μg and 1208.04 ​± ​417.9 ​μg of TAF in the skin after 24 ​h. Pharmacokinetic experiments in rats demonstrated a fast metabolization of TAF into tenofovir, with a rapid elimination of the metabolite from the plasma. The MAPs described in this work could be used as an alternative to current oral treatments for HIV management

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

Inisiasi dan pengembangan produk handsanitizer pada center of excellence Fakultas Farmasi Universitas Hasanuddin sebagai upaya pengembangan usaha intelektual kampus

PPUPIK is a community service program for 3 years. The purpose of this activity is to produce the intellectual products from the Faculty of Pharmacy UNHAS, especially Hand sanitizer and Disinfectant products, so that the Center of Excellence of the Faculty of Pharmacy UNHAS (CoE-FFUH) would become an independent business unit that able to support UNHAS' role as PTNBH. The specific target for this first year is the initiation of the development of a production unit of hand sanitizer and disinfectant products at CoE-FFUH. The initiation consists of the determination of documents for the production process, determination of product packaging material and designs, and also pilot-scale production for limited sales. As for the following year, hopefully, this product will be able to obtain a distribution permit for household health supplies (PKRT) so that the commercialization of licensed products can be carried out legally and able to produce more types of PKRT products

Ring inserts as a useful strategy to prepare tip-loaded microneedles for long-acting drug delivery with application in HIV pre-exposure prophylaxis

The role of microneedle array patches (MAPs) and, in particular, dissolving MAPs in transdermal drug delivery has increased exponentially over the last decade. MAPs are able to form drug depots in the viable skin from where poorly soluble drugs dissolve in a long-acting fashion, showing promise in the management of multiple diseases. The manufacture of these systems can present some challenges, including the presence of bubbles in the baseplates and consequent lack of uniformity in microneedle formation and drug content. Here, we present a simple method based on ring inserts to produce tip-loaded MAPs using the antiretroviral drug cabotegravir sodium (CAB). The obtained MAPs presented a high uniformity in terms of microneedle formation, and a suitable insertion capability, as per the mechanical characterisation performed. An optimisation based on design of experiments revealed that centrifugation parameters had a significant impact on the skin deposition of the MAPs in excised neonatal porcine skin using Franz cells, with values ranging from 62.24 ± 47.13 µg to 174.13 ± 41.10 µg of CAB. Pharmacokinetic studies carried out in rats evidenced the capacity of the MAPs to maintain therapeutic plasma levels of CAB for 14 days, with Tmax values reached between 5 and 8 days

Hydrogel-forming microarray patches with cyclodextrin drug reservoirs for long-acting delivery of poorly soluble cabotegravir sodium for HIV Pre-Exposure Prophylaxis

Hydrogel-forming microarray patches (HF-MAPs) offer minimally invasive, pain-free and prolonged drug delivery. These devices are designed to be self-administered and self-disabling, avoiding contaminated sharps waste generation. Cabotegravir sodium (CAB-Na) is a poorly soluble anti- human immunodeficiency virus (HIV) drug for the treatment and pre-exposure prophylaxis of HIV infection that lends itself to depot formation following intradermal delivery but presents significant challenges when delivered via HF-MAPs, whose nature is aqueous. Herein, we have investigated, for the first time, the use of hydroxypropyl-β-cyclodextrin (HP-β-CD) to enhance the solubility of CAB-Na, and its effect on intradermal delivery via HF-MAPs. Accordingly, tablet reservoirs containing CAB-Na and HP-β-CD were formulated. These novel reservoirs were combined with two different HF-MAP formulations (MAP1 (Gantrez S97® + poly (ethylene glycol) 10,000 + Na2CO3) and MAP2 (poly (vinyl pyrrolidone) 58 kDa + poly (vinyl alcohol) 85–120 kDa + citric acid)) to form fully integrated MAP devices which were tested in both ex vivo and in vivo settings. Ex vivo skin deposition results for MAP1 and MAP2 showed that 141 ± 40 μg and 342 ± 34 μg of CAB-Na was deposited into 0.5 cm2 of excised neonatal porcine skin after 24 h, respectively. Based on these findings, the in vivo pharmacokinetics of MAP2 were investigated over 28 days using a Sprague-Dawley rat model. After 24 h patch application, MAP2 demonstrated an extended drug release profile and an observed Cmax of 53.4 ± 10.16 μg/mL, superior to that of an FDA-approved CAB-nanosuspension administered via intramuscular application (Cmax of 43.6 ± 5.3 μg/mL). Consequently, this tablet integrated MAP device is considered to be a viable option for the intradermal delivery of hydrophobic anti-HIV drugs