Displaying publications 81 - 100 of 162 in total

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  1. Fulltext Antimycobacterial susceptibility evaluation of rifampicin and isoniazid benz-hydrazone in biodegradable polymeric nanoparticles against Mycobacterium tuberculosis H37Rv strain
    Hakkimane SS, Shenoy VP, Gaonkar SL, Bairy I, Guru BR
    Int J Nanomedicine, 2018;13:4303-4318.
    PMID: 30087562 DOI: 10.2147/IJN.S163925
    INTRODUCTION: Tuberculosis (TB) is the single largest infectious disease which requires a prolonged treatment regime with multiple drugs. The present treatment for TB includes frequent administration of a combination of four drugs for a duration of 6 months. This leads to patient's noncompliance, in addition to developing drug-resistant strains which makes treatment more difficult. The formulation of drugs with biodegradable polymeric nanoparticles (NPs) promises to overcome this problem.

    MATERIALS AND METHODS: In this study, we focus on two important drugs used for TB treatment - rifampicin (RIF) and isoniazid (INH) - and report a detailed study of RIF-loaded poly lactic-co-glycolic acid (PLGA) NPs and INH modified as INH benz-hydrazone (IH2) which gives the same therapeutic effect as INH but is more stable and enhances the drug loading in PLGA NPs by 15-fold compared to INH. The optimized formulation was characterized using particle size analyzer, scanning electron microscopy and transmission electron microscopy. The drug release from NPs and stability of drug were tested in different pH conditions.

    RESULTS: It was found that RIF and IH2 loaded in NPs release in a slow and sustained manner over a period of 1 month and they are more stable in NPs formulation compared to the free form. RIF- and IH2-loaded NPs were tested for antimicrobial susceptibility against Mycobacterium tuberculosis H37Rv strain. RIF loaded in PLGA NPs consistently inhibited the growth at 70% of the minimum inhibitory concentration (MIC) of pure RIF (MIC level 1 µg/mL), and pure IH2 and IH2-loaded NPs showed inhibition at MIC equivalent to the MIC of INH (0.1 µg/mL).

    CONCLUSION: These results show that NP formulations will improve the efficacy of drug delivery for TB treatment.

    Matched MeSH terms: Drug Compounding
  2. Fulltext Application of supercritical antisolvent method in drug encapsulation: a review
    Kalani M, Yunus R
    Int J Nanomedicine, 2011;6:1429-42.
    PMID: 21796245 DOI: 10.2147/IJN.S19021
    The review focuses on the application of supercritical fluids as antisolvents in the pharmaceutical field and demonstrates the supercritical antisolvent method in the use of drug encapsulation. The main factors for choosing the solvent and biodegradable polymer to produce fine particles to ensure effective drug delivery are emphasized and the effect of polymer structure on drug encapsulation is illustrated. The review also demonstrates the drug release mechanism and polymeric controlled release system, and discusses the effects of the various conditions in the process, such as pressure, temperature, concentration, chemical compositions (organic solvents, drug, and biodegradable polymer), nozzle geometry, CO(2) flow rate, and the liquid phase flow rate on particle size and its distribution.
    Matched MeSH terms: Drug Compounding/methods*
  3. Investigation of Filler Effects on the Compounding of Freeze-dried Orodispersible Tablets Containing Annona muricata Extract
    Azman SEN, Abd Razak FS, Kamal WHBW, Zheng GK, Ming LC, Uddin AH, et al.
    Int J Pharm Compd, 2020 11 21;24(6):509-514.
    PMID: 33217741
    Orally disintegrating tablets are a solid dosage form that will disintegrate rapidly within 3 minutes upon contact with saliva. Fillers or diluents are excipients that are used to make up the volume of orally disintegrating tablets, and some might act as a disintegrant or binder that will affect the physical properties of orally disintegrating tablets. The objective of this study was to formulate and evaluate physical properties of orally disintegrating tablets containing Annona muricata leaves extract by a freeze-drying method using different fillers at different concentrations. In this study, fifteen formulations of orally disintegrating tablets were prepared by a freeze-drying method with different fillers such as starch, lactose, microcrystalline cellulose, StarLac, and CombiLac at 5%, 10%, and 15%. The orally disintegrating tablets were evaluated for hardness, thickness, weight variation, friability, and disintegration time test. The optimum formulation was chosen and incorporated with Annona muricata leaves extract. The results obtained in this work indicated that Formulation 3, with 15% starch, was the most optimum formulation due to the shortest disintegration time (21.08 seconds ± 4.24 seconds), and all the physical tests were within the acceptable range. The orally disintegrating tablets containing Annona muricata leaves extract possessed antioxidant activity and stable at least for 3 months under 60°C and 75% relative humidity.
    Matched MeSH terms: Drug Compounding
  4. Comparison of Disintegrant-addition Methods on the Compounding of Orodispersible Tablets
    Mahesparan VA, Bin Abd Razak FS, Ming LC, Uddin AH, Sarker MZI, Bin LK
    Int J Pharm Compd, 2020 3 21;24(2):148-155.
    PMID: 32196477
    Orodispersible tablets disintegrate rapidly (within 3 minutes) in the oral cavity and release the medicament before swallowing. The mode of disintegrant addition might affect the properties of orodispersible tablets. The objective of this study was to formulate and evaluate orodispersible tablets by studying different modes of disintegration addition with varying concentrations of disintegrants. The wet granulation method was used to produce the orodispersible tablets. Two methods of disintegration addition were compared (i.e., intragranular, extragranular). Three disintegrants (i.e., cornstarch, sodium starch glycolate, crospovidone) were used at three levels (5%, 10%, and 15%) in the study. The formulations were tested for the powder flowability (angle of repose) and characterized physically (hardness, weight, thickness, friability, disintegration time). The mangosteen pericarp extract was used as a model active pharmaceutical ingredient to be incorporated into the optimum formulation. It was observed that the extragranular method produced granules with better flowability compared to that of the intragranular method. Crospovidone was found as the most efficient disintegrant among the three. The optimum formulation selected was one with the highest concentration of crospovidone (15%), which showed the fastest disintegration time. The mode of disintegrant addition into the orodispersible tablets formulation was found to show a marked difference in the disintegration, as well as other physical characteristics of the orodispersible tablets where the extragranular mode of addition showed better property, which caused the orodispersible tablets to disintegrate the fastest.
    Matched MeSH terms: Drug Compounding/methods*
  5. Investigation of the Effects of Excipients in the Compounding of Amlodipine Besylate Orally Disintegrating Tablets
    Azmi NHS, Ming LC, Uddin ABMH, Sarker ZI, Bin LK
    Int J Pharm Compd, 2022 1 27;26(1):80-87.
    PMID: 35081048
    Oral drug delivery has been recognized as the most desirable drug administration method among other drug delivery routes due to its ease of administration, long shelf life, and low cost. Orally disintegrating tablets disintegrate within seconds in the mouth without the need of water for swallowing. This unique feature of orally disintegrating tablets is favorable to special populations such as geriatric and pediatric patients. Formulation optimization is significant to obtain the optimal combination of tablet constituents, as the tablet composition is influential on dosage-form characteristics. The objective of this study was to investigate the effect of different types of fillers and percentage on the physical properties of orally disintegrating tablets by using amlodipine as the model drug. Blank orally disintegrating tablets containing different fillers, namely, Sorbolac 400, Granulac 200, and CombiLac with different percentages, were prepared using the wet granulation method and were evaluated based on weight variation, hardness, thickness, friability, and disintegration time. Formulation 5 that consists of 25% Granulac 200 showed the optimal result among all formulations with the fastest disintegration time (96.17 s Å} 18.40) and sufficient tablet hardness (4.59 kg Å} 0.70). Hence, formulation 5 was selected as the optimal formulation and incorporated with amlodipine. From this study, it can be concluded that excipients have an essential role in determining the physical properties of orally disintegrating tablets.
    Matched MeSH terms: Drug Compounding
  6. Anti-inflammatory and analgesic activity of novel oral aspirin-loaded nanoemulsion and nano multiple emulsion formulations generated using ultrasound cavitation
    Tang SY, Sivakumar M, Ng AM, Shridharan P
    Int J Pharm, 2012 Jul 1;430(1-2):299-306.
    PMID: 22503988 DOI: 10.1016/j.ijpharm.2012.03.055
    The present study investigated the anti-inflammatory and analgesic activities of novel aspirin oil-in-water (O/W) nanoemulsion and water-in-oil-in-water (W/O/W) nano multiple emulsion formulations generated using ultrasound cavitation techniques. The anti-inflammatory activities of nanoemulsion and nano multiple emulsion were determined using the λ-carrageenan-induced paw edema model. The analgesic activities of both nanoformulations were determined using acetic acid-induced writhing response and hot plate assay. For comparison, the effect of pretreatment with blank nanoemulsion and reference aspirin suspension were also studied for their anti-inflammatory and antinociceptive activities. The results showed that oral administration of nanoemulsion and nano multiple emulsion containing aspirin (60 mg/kg) significantly reduced paw edema induced by λ-carrageenan injection. Both nanoformulations decreased the number of abdominal constriction in acetic acid-induced writhing model. Pretreatment with nanoformulations led to a significant increase in reaction time in hot plate assay. Nanoemulsion demonstrated an enhanced anti-inflammatory and analgesic effects compared to reference suspension while nano multiple emulsion exhibited a mild inhibitory effects in the three experimental animal model tests. The results obtained for nano multiple emulsion were relatively lower than reference. However, administration of blank nanoemulsion did not alter the nociceptive response significantly though it showed slight anti-inflammatory effect. These experimental studies suggest that nanoemulsion and nano multiple emulsion produced a pronounced anti-inflammatory and analgesic effects in rats and may be candidates as new nanocarriers for pharmacological NSAIDs in the treatment of inflammatory disorders and alleviating pains.
    Matched MeSH terms: Drug Compounding
  7. The transit of dosage forms through the small intestine
    Yuen KH
    Int J Pharm, 2010 Aug 16;395(1-2):9-16.
    PMID: 20478371 DOI: 10.1016/j.ijpharm.2010.04.045
    The human small intestine, with its enormous absorptive surface area, is invariably the principal site of drug absorption. Hence, the residence time of a dosage form in this part of the gut can have a great influence on the absorption of the contained drug. Various methods have been employed to monitor the gastrointestinal transit of pharmaceutical dosage forms, but the use of gamma-scintigraphy has superceded all the other methods. However, careful consideration of the time interval for image acquisition and proper analysis of the scintigraphic data are important for obtaining reliable results. Most studies reported the mean small intestinal transit time of various dosage forms to be about 3-4h, being closely similar to that of food and water. The value does not appear to be influenced by their physical state nor the presence of food, but the timing of food intake following administration of the dosage forms can influence the small intestinal transit time. While the mean small intestinal transit time is quite consistent among dosage forms and studies, individual values can vary widely. There are differing opinions regarding the effect of density and size of dosage forms on their small intestinal transit properties. Some common excipients employed in pharmaceutical formulations can affect the small intestinal transit and drug absorption. There is currently a lack of studies regarding the effects of excipients, as well as the timing of food intake on the small intestinal transit of dosage forms and drug absorption.
    Matched MeSH terms: Drug Compounding
  8. Technical aspects of preparing PEG-PLGA nanoparticles as carrier for chemotherapeutic ‎agents by nanoprecipitation method
    Almoustafa HA, Alshawsh MA, Chik Z
    Int J Pharm, 2017 Nov 25;533(1):275-284.
    PMID: 28943210 DOI: 10.1016/j.ijpharm.2017.09.054
    Nanoprecipitation is a simple and increasingly trending method for nanoparticles preparation. The self-assembly feature of poly (ethylene glycol)-poly (lactide-co-glycolic acid) (PEG-PLGA) amphiphilic copolymer into a nanoparticle and its versatile structure makes nanoprecipitation one of the best methods for its preparation. The aim of this study is to review currently available literature for standard preparation of PEG-PLGA nanoparticles using nanoprecipitation technique in order to draw conclusive evidenceto draw conclusive evidence that can guide researchers during formulation development. To achieve this, three databases (Web of Science, Scopus and PubMed) were searched using relevant keywords and the extracted articles were reviewed based on defined inclusion and exclusion criteria. Data extraction and narrative analysis of the obtained literature was performed when appropriate, along with our laboratory observations to support those claims wherever necessary. As a result of this analysis, reports that matched our criteria conformed to the general facts about nanoprecipitation techniques such as simplicity in procedure, low surfactants requirement, narrow size distribution, and low resulting concentrations. However, these reports showed interesting advantages for using PEG-PLGA as they are frequently reported to be freeze-dried and active pharmaceutical ingredients (APIs) with low hydrophobicity were reported to successfully be encapsulated in the particles.
    Matched MeSH terms: Drug Compounding/methods*
  9. High-capacity glycol chitosan-based nanoemulsion for efficient delivery of disulfiram
    Abd Kadir E, Uchegbu IF, Schätzlein AG
    Int J Pharm, 2023 Jun 10;640:123036.
    PMID: 37169106 DOI: 10.1016/j.ijpharm.2023.123036
    Disulfiram (DS) is an anti-alcoholism drug capable of acting against important and hard-to-treat cancers. The drug's relative instability and variable absorption/distribution have led to its variable pharmacokinetics and suboptimal exposure. Hence, it was hypothesised that a nano-enabled form of DS might be able to overcome such limitations. Encapsulation of the labile DS was achieved with quaternary ammonium palmitoyl glycol chitosan (GCPQ) to form a high-capacity, soybean oil-based DS-GCPQ nanoemulsion. DS-GCPQ showed capability of oil-loading up to 50% v/v for a stable entrapment of high drug content. With increasing oil content (10 to 50% v/v), the mean particle size and polydispersity index were also increased (166 to 351 nm and 0.14 to 0.22, respectively) for a given amount of GCPQ. Formulations showed a highly positive particle surface charge (50.9 ± 1.3 mV), contributing to the colloidal stability of the individual particles. DS-GCPQ showed marked cytotoxicity against pancreatic cancer cell lines with enhanced activity in the presence of copper. An intravenous pharmacokinetic study of DS-GCPQ in vivo showed improved plasma drug stability with a DS half-life of 17 min. Prolonged survival was seen in tumour-bearing animals treated with DS-GCPQ supplemented with copper. In conclusion, DS-GCPQ nanoemulsion has the potential to be developed further for cancer therapeutic purposes.
    Matched MeSH terms: Drug Compounding
  10. Differentiation of patented crystalline glucosamine sulfate from other glucosamine preparations will optimize osteoarthritis treatment
    Saengnipanthkul S, Waikakul S, Rojanasthien S, Totemchokchyakarn K, Srinkapaibulaya A, Cheh Chin T, et al.
    Int J Rheum Dis, 2019 Mar;22(3):376-385.
    PMID: 28332780 DOI: 10.1111/1756-185X.13068
    Symptomatic slow-acting drugs for osteoarthritis (SYSADOAs) are recommended for the medium- to long-term management of knee osteoarthritis (OA) due to their abilities to control pain, improve function and delay joint structural changes. Among SYSADOAs, evidence is greatest for the patented crystalline glucosamine sulfate (pCGS) formulation (Mylan). Glucosamine is widely available as glucosamine sulfate (GS) and glucosamine hydrochloride (GH) preparations that vary substantially in molecular form, pharmaceutical formulation and dose regimen. Only pCGS is given as a highly bioavailable once-daily dose (1500 mg), which consistently delivers the plasma levels of around 10 μmol/L required to inhibit interleukin-1-induced expression of genes involved in the pathophysiology of joint inflammation and tissue destruction. Careful consideration of the evidence base reveals that only pCGS reliably provides a moderate effect size on pain that is higher than paracetamol and equivalent to non-steroidal anti-inflammatory drugs (NSAIDs), while non-crystalline GS and GH fail to reach statistical significance for pain reduction. Chronic administration of pCGS has disease-modifying effects, with a reduction in need for total joint replacement lasting for 5 years after treatment cessation. Pharmacoeconomic studies of pCGS demonstrate long-term reduction in additional pain analgesia and NSAIDs, with a 50% reduction in costs of other OA medication and healthcare consultations. Consequently, pCGS is the logical choice, with demonstrated medium-term control of pain and lasting impact on disease progression. Physician and patient education on the differentiation of pCGS from other glucosamine formulations will help to improve treatment selection, increase treatment adherence, and optimize clinical benefit in OA.
    Matched MeSH terms: Drug Compounding
  11. Fulltext Characterization of encapsulated ginger essential oils and its antimicrobial properties
    Tengku Shafazila Tengku Saharuddin, Lailatun Nazirah Ozair, Ayuni Shahira Zulkifli, Nursarah Syazwani Hairul Shah, Nur Syafiqah Sahidan
    Journal of Academia Universiti Teknologi MARA Negeri Sembilan, 2020;8(1):1-6.
    MyJurnal
    Ginger essential oils (GEO) are natural products with antibacteria properties consisting of many different volatile
    compounds have high potential to be used in many applications. In this study, the ginger GEO was successfully
    encapsulated in chitosan as a carrier agent using a spray drying technique. The extraction of Zingiber officinale
    (ginger) essential oil is performed by steam distillation method. The GEO was encapsulated in chitosan as a carrier
    agents at 1:3, GEO:chitosan ratio by using spray drying technique. GEO together with encapsulated GEO were
    further assayed for antimicrobial activity by disc-diffusion method. For characterization of encapsulated GEO,
    Fourier transform infrared spectroscopy (FTIR) and Field emission scanning electron microscopy (FESEM) were
    used. FTIR analysis revealed that there was no existence of a new functional group in the encapsulated GEO
    showing that there is only physical interaction between GEO and chitosan. Besides, FESEM analysis showed the
    encapsulated GEO were in micro in sizes and possessed spherical shape with smooth and porous surface.
    Furthermore, Both GEO and encapsulated GEO showed in vitro antimicrobial activity against Escheriachia coli,
    Pseudomonas aeruginosa, Staphylococcus aureus and Salmonella typhi with encapsulated GEO possessed higher in
    the activities for all studied bacteria compared to GEO. The encapsulated GEO demonstrated a superior performance
    against Salmonella typhi with the inhibition zone of 22.5 mm compared to GEO only 13.5 mm. The results obtained
    indicated that due to the volatility and instability of the GEO when exposed to environmental factors, its encapsulation considerably improve and enhanced its performance.
    Matched MeSH terms: Drug Compounding
  12. Chitosan-Based Agronanofungicides as a Sustainable Alternative in the Basal Stem Rot Disease Management
    Maluin FN, Hussein MZ, Azah Yusof N, Fakurazi S, Idris AS, Zainol Hilmi NH, et al.
    J Agric Food Chem, 2020 Apr 15;68(15):4305-4314.
    PMID: 32227887 DOI: 10.1021/acs.jafc.9b08060
    The rise of environmental and health concerns due to the excessive use of the conventional fungicide urges the search for sustainable alternatives of agronanofungicides where the latter is aimed to enhance plant uptake and minimize the volatilization, leaching, and runoff of fungicides. With this in mind, fungicides of hexaconazole and/or dazomet were encapsulated into chitosan nanoparticles for the formulation of chitosan-based agronanofungicides. In the present study, chitosan nanoparticles (2 nm), chitosan-hexaconazole nanoparticles (18 and 168 nm), chitosan-dazomet nanoparticles (7 and 32 nm), and chitosan-hexaconazole-dazomet nanoparticles (5 and 58 nm) were synthesized and used as potent antifungal agents in combating the basal stem rot (BSR) disease caused by Ganoderma boninense in which they were evaluated via an artificial inoculation of oil palm seedlings with the rubber woodblock, which was fully colonized with the fungal Ganoderma boninense mycelium. The results revealed that chitosan nanoparticles could act as dual modes of action, which are themselves as a biocide or as a nanocarrier for the existing fungicides. In addition, the particle size of the chitosan-based agronanofungicides plays a crucial role in suppressing and controlling the disease. The synergistic effect of the double-fungicide system of 5 nm chitosan-hexaconazole-dazomet nanoparticles can be observed as the system showed the highest disease reduction with 74.5%, compared to the untreated infected seedlings.
    Matched MeSH terms: Drug Compounding
  13. Pharmacokinetics and tissue distribution of an orally administered mucoadhesive chitosan-coated amphotericin B-Loaded nanostructured lipid carrier (NLC) in rats
    Tan JSL, Roberts C, Billa N
    J Biomater Sci Polym Ed, 2020 02;31(2):141-154.
    PMID: 31612804 DOI: 10.1080/09205063.2019.1680926
    Oral delivery of amphotericin B (AmpB) is desirable because it provides a more patient-friendly mode of administration compared to the current delivery approach akin with the marketed AmpB formulations. The goal of the study was to investigate the pharmacokinetics and tissue distribution of orally administered chitosan-coated AmpB-loaded nanostructured lipid carriers (ChiAmpB NLC) administered to Sprague Dawley rats at a dose of 15 mg/kg. Orally administered ChiAmpB NLC resulted in a two-fold increase in the area under the curve (AUC0-∞) compared to the uncoated AmpB NLC and marketed Amphotret®. This enhanced bioavailability of AmpB suggests prolonged transit and retention of ChiAmpB NLC within the small intestine through mucoadhesion and subsequent absorption by the lymphatic pathway. The results show that mean absorption and residence times (MAT & MRT) were significantly higher from ChiAmpB NLC compared to the other two formulations, attesting to the mucoadhesive effect. The ChiAmpB NLC presented a lower nephrotic accumulation with preferential deposition in liver and spleen. Thus, the limitations of current marketed IV formulations of AmpB are potentially addressed with the ChiAmpB NLC in addition to utilizing this approach for targeting internal organs in visceral leishmaniasis.
    Matched MeSH terms: Drug Compounding
  14. Sodium carboxymethyl cellulose hydrogels containing reduced graphene oxide (rGO) as a functional antibiofilm wound dressing
    Ali NH, Amin MCIM, Ng SF
    J Biomater Sci Polym Ed, 2019 06;30(8):629-645.
    PMID: 30896336 DOI: 10.1080/09205063.2019.1595892
    Biofilms comprise bacteria attached to wound surfaces and are major contributors to non-healing wounds. It was found that the increased resistance of biofilms to antibiotics allows wound infections to persist chronically in spite of antibiotic therapy. In this study, the reduced form of graphene oxide (rGO) was explored as plausible antibiofilm agents. The rGO was synthesized via reducing the functional groups of GO. Then, rGO were characterized using zetasizer, X-ray photoelectron spectroscopy, UV-Vis spectroscopy and FESEM. The rGO were then formulated into sodium carboxymethyl cellulose (NaCMC) hydrogels to form rGO hydrogel and tested for antibiofilm activities in vitro using XTT test, and in vivo biofilm formation assay using nematodes C. elegans. Reduced GO hydrogel was successfully formed by reducing the functional groups of GO, and a reduction of up to 95% of functional groups was confirmed with X-ray photoelectron spectroscopy analysis. XTT tests confirmed that rGO hydrogels reduced biofilm formation by S. aureus (81-84%) and P. aeruginosa (50-62%). Fluorescence intensity also confirmed that rGO hydrogel can inhibit biofilm bacteria in C. elegans experiments. This study implied that rGO hydrogel is an effective antibiofilm agent for infected wounds.
    Matched MeSH terms: Drug Compounding/methods
  15. Harnessing amphiphilic polymeric micelles for diagnostic and therapeutic applications: Breakthroughs and bottlenecks
    Kaur J, Mishra V, Singh SK, Gulati M, Kapoor B, Chellappan DK, et al.
    J Control Release, 2021 06 10;334:64-95.
    PMID: 33887283 DOI: 10.1016/j.jconrel.2021.04.014
    Amphiphilic block copolymers are widely utilized in the design of formulations owing to their unique physicochemical properties, flexible structures and functional chemistry. Amphiphilic polymeric micelles (APMs) formed from such copolymers have gained attention of the drug delivery scientists in past few decades for enhancing the bioavailability of lipophilic drugs, molecular targeting, sustained release, stimuli-responsive properties, enhanced therapeutic efficacy and reducing drug associated toxicity. Their properties including ease of surface modification, high surface area, small size, and enhanced permeation as well as retention (EPR) effect are mainly responsible for their utilization in the diagnosis and therapy of various diseases. However, some of the challenges associated with their use are premature drug release, low drug loading capacity, scale-up issues and their poor stability that need to be addressed for their wider clinical utility and commercialization. This review describes comprehensively their physicochemical properties, various methods of preparation, limitations followed by approaches employed for the development of optimized APMs, the impact of each preparation technique on the physicochemical properties of the resulting APMs as well as various biomedical applications of APMs. Based on the current scenario of their use in treatment and diagnosis of diseases, the directions in which future studies need to be carried out to explore their full potential are also discussed.
    Matched MeSH terms: Drug Compounding
  16. Fulltext Mechanism-based selection of stabilization strategy for amorphous formulations: Insights into crystallization pathways
    Edueng K, Mahlin D, Larsson P, Bergström CAS
    J Control Release, 2017 06 28;256:193-202.
    PMID: 28412224 DOI: 10.1016/j.jconrel.2017.04.015
    We developed a step-by-step experimental protocol using differential scanning calorimetry (DSC), dynamic vapour sorption (DVS), polarized light microscopy (PLM) and a small-scale dissolution apparatus (μDISS Profiler) to investigate the mechanism (solid-to-solid or solution-mediated) by which crystallization of amorphous drugs occurs upon dissolution. This protocol then guided how to stabilize the amorphous formulation. Indapamide, metolazone, glibenclamide and glipizide were selected as model drugs and HPMC (Pharmacoat 606) and PVP (K30) as stabilizing polymers. Spray-dried amorphous indapamide, metolazone and glibenclamide crystallized via solution-mediated nucleation while glipizide suffered from solid-to-solid crystallization. The addition of 0.001%-0.01% (w/v) HPMC into the dissolution medium successfully prevented the crystallization of supersaturated solutions of indapamide and metolazone whereas it only reduced the crystallization rate for glibenclamide. Amorphous solid dispersion (ASD) formulation of glipizide and PVP K30, at a ratio of 50:50% (w/w) reduced but did not completely eliminate the solid-to-solid crystallization of glipizide even though the overall dissolution rate was enhanced both in the absence and presence of HPMC. Raman spectroscopy indicated the formation of a glipizide polymorph in the dissolution medium with higher solubility than the stable polymorph. As a complementary technique, molecular dynamics (MD) simulations of indapamide and glibenclamide with HPMC was performed. It was revealed that hydrogen bonding patterns of the two drugs with HPMC differed significantly, suggesting that hydrogen bonding may play a role in the greater stabilizing effect on supersaturation of indapamide, compared to glibenclamide.
    Matched MeSH terms: Drug Compounding
  17. Tableting Properties and Compression Models of Labisia pumila Tablets
    Etti CJ, Yusof YA, Chin NL, Mohd Tahir S
    J Diet Suppl, 2017 Mar 04;14(2):132-145.
    PMID: 27487244
    The tableting properties of Labisia pumila herbal powder, which is well known for its therapeutic benefits was investigated. The herbal powder was compressed into tablets using a stainless steel cylindrical uniaxial die of 13-mm- diameter with compaction pressures ranging from 7 to 25 MPa. Two feed weights, 0.5 and 1.0 g were used to form tablets. Some empirical models were used to describe the compressibility behavior of Labisia pumila tablets. The strength and density of tablets increased with increase in compaction pressure and resulted in reduction in porosity of the tablets. Smaller feeds, higher forces and increase in compaction pressure, contributed to more coherent tablets. These findings can be used to enhance the approach and understanding of tableting properties of Labisia pumila herbal powder tablets.
    Matched MeSH terms: Drug Compounding/methods*
  18. Development and Standardization of Moringa oleifera Leaves as a Natural Dietary Supplement
    Ali MA, Yusof YA, Chin NL, Ibrahim MN, Muneer S
    J Diet Suppl, 2019;16(1):66-85.
    PMID: 29469600 DOI: 10.1080/19390211.2018.1429517
    Moringa oleifera leaves were selected as a model due to their hundreds of health benefits. On the other hand, the powder of these leaves has exhibited poor flowability, low tensile strength, bitter taste, poor dissolution rate, and lack of information regarding dosage. These are the common hurdles and limitations in the adaptation of herbal-based medications. Therefore, a comprehensive study was planned to introduce herbal-based medicines into mainstream medicines by standardization according to the U.S. Food and Drug Administration (FDA) and international pharmaceutical standards. A Simplex Lattice Design (SLD) of Design Expert 8.0 software was used to formulate different concentrations of superdisintegrant, binder/diluent, and sweeteners. An Instron Universal Testing machine coupled with a 13 mm stainless cylindrical die was used to manufacture tablets by means of direct compression method at 20 kN applied force. Therefore, selection of excipients was made on the basis of their tensile strength, flowability, and taste-masking properties. Optimum formulation was tested on rabbits for toxicity and growth rate. All formulated tablets were evaluated on standard parameters for orally disintegrating tablets described by the Food and Drug Authority (U.S.). The optimum formulation fulfills all standard parameters such as hardness, disintegration time, friability, and dissolution rate. The present formulation showed no toxicity when tested on rabbits. The present study provides a fundamental understanding of the tableting characteristics of natural medicines. The present study provides information that will help to overcome the challenges.
    Matched MeSH terms: Drug Compounding/methods*
  19. Fulltext Microencapsulation of fish oil using supercritical antisolvent process
    Karim FT, Ghafoor K, Ferdosh S, Al-Juhaimi F, Ali E, Yunus KB, et al.
    J Food Drug Anal, 2017 Jul;25(3):654-666.
    PMID: 28911651 DOI: 10.1016/j.jfda.2016.11.017
    In order to improve the encapsulation process, a newly supercritical antisolvent process was developed to encapsulate fish oil using hydroxypropyl methyl cellulose as a polymer. Three factors, namely, temperature, pressure, and feed emulsion rate were optimized using response surface methodology. The suitability of the model for predicting the optimum response value was evaluated at the conditions of temperature at 60°C, pressure at 150 bar, and feed rate at 1.36 mL/min. At the optimum conditions, particle size of 58.35 μm was obtained. The surface morphology of the micronized fish oil was also evaluated using field emission scanning electron microscopy where it showed that particles formed spherical structures with no internal voids. Moreover, in vitro release of oil showed that there are significant differences of release percentage of oil between the formulations and the results proved that there was a significant decrease in the in vitro release of oil from the powder when the polymer concentration was high.
    Matched MeSH terms: Drug Compounding
  20. Effects of Accelerated Storage on the Quality of Kenaf Seed Oil in Chitosan-Coated High Methoxyl Pectin-Alginate Microcapsules
    Leong MH, Tan CP, Nyam KL
    J Food Sci, 2016 Oct;81(10):C2367-C2372.
    PMID: 27635525 DOI: 10.1111/1750-3841.13442
    The objective of this research was to study the oxidative stability and antioxidant properties of microencapsulated kenaf (Hibiscus cannabinus L.) seed oil (MKSO) produced by co-extrusion technology upon accelerated storage. The combination of sodium alginate, high methoxyl pectin, and chitosan were used as shell materials. The oxidative stability of the kenaf seed oil was determined by iodine value, peroxide value, p-Anisidine value, total oxidation (TOTOX), thiobarbituric acid reactive substances assay, and free fatty acid content. Total phenolic content, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) cation radical-scavenging assay and 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay were used to examine the antioxidant properties of oils. Oxidative stability tests showed that bulk kenaf seed oil (BKSO) was oxidized significantly higher (P < 0.05) than MKSO. The total increment of TOTOX value of BKSO was 165.93% significantly higher (P < 0.05) than MKSO. Co-extrusion technology has shown to be able to protect kenaf seed oil against lipid oxidation and delay the degradation of natural antioxidants that present in oil during storage.
    Matched MeSH terms: Drug Compounding*
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