Displaying publications 101 - 120 of 405 in total

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  1. Sheshala R, Khan N, Darwis Y
    Chem Pharm Bull (Tokyo), 2011;59(8):920-8.
    PMID: 21804234
    The aims of the present research were to mask the intensely bitter taste of sumatriptan succinate and to formulate orally disintegrating tablets (ODTs) of the taste masked drug. Taste masking was performed by coating sumatriptan succinate with Eudragit EPO using spray drying technique. The resultant microspheres were evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentrations of superdisintegrants and compressed using direct compression method followed by sublimation technique. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. All the tablet formulations disintegrated in vitro within 37-410 s. The optimized formulation containing 5% Kollidon CL-SF released more than 90% of the drug within 15 min and the release was comparable to that of commercial product (Suminat®). In human volunteers, the optimized formulation was found to have a pleasant taste and mouth feel and disintegrated in the oral cavity within 41 s. The optimized formulation was found to be stable and bioequivalent with Suminat®.
    Matched MeSH terms: Administration, Oral
  2. Rehman U, Sarfraz RM, Mahmood A, Hussain Z, Thu HE, Zafar N, et al.
    Curr Drug Deliv, 2021 Feb 11.
    PMID: 33583374 DOI: 10.2174/1567201818666210212085912
    BACKGROUND: Despite exhibiting promising anticancer potential, the clinical significance of capecitabine (a potent prodrug of 5-fluorouracil used for treatment of colorectal cancer) is limited owing to its acidic and enzymatic hydrolysis, lower absorption following the oral administration, poor bioavailability, short plasma half-life and poor patient compliance.

    OBJECTIVES: The present study was aimed to fabricate the capecitabine as smart pH-responsive hydrogel network to efficiently facilitate its oral delivery while shielding its stability in the gastric media.

    METHODS: The smart pH sensitive HP-β-CD/agarose-g-poly(MAA) hydrogel network was developed using an aqueous free radical polymerization technique. The developed hydrogels were characterized for drug-loading efficiency, structural and compositional features, thermal stability, swelling behaviour, morphology, physical form, and release kinetics. The pH-responsive behaviour of developed hydrogels was established by conducting the swelling and release behaviour at different pH values (1.2 and 7.4), demonstrating significantly higher swelling and release at pH 7.4 as compared with pH 1.2. The capecitabine-loaded hydrogels were also screened for acute oral toxicity in animals by analysing the body weight, water and food intake, dermal toxicity, ocular toxicity, biochemical analysis, and histological examination.

    RESULTS: The characteristic evaluations revealed that capecitabine (anticancer agent) was successfully loaded into the hydrogel network. Capecitabine loading was ranged from 71.22% to 90.12%. An interesting feature of hydrogel was its pH-responsive behaviour which triggers release at basic pH (94.25%). Optimum swelling (95%) was seen at pH 7.4. Based upon regression coefficient R2 (0.96 - 0.99) best fit model was zero order. The extensive toxicity evaluations evidenced good safety profile with no signs of oral, dermal or ocular toxicities, as well as no variations in blood parameters and histology of vital organs.

    CONCLUSION: Our findings conclusively evinced that the developed hydrogel exhibited excellent pharmaceutical and therapeutic potential and thus can be employed as pH-responsive system for controlled delivery of anticancer agents.

    Matched MeSH terms: Administration, Oral
  3. Suresh N, Nagendrababu V, Koteeswaran V, Haritha JS, Swetha SD, Varghese A, et al.
    Int Endod J, 2021 Feb;54(2):198-209.
    PMID: 32976660 DOI: 10.1111/iej.13416
    AIM: This randomized, double-blinded, clinical trial evaluated the effect of oral premedication of piroxicam, prednisolone, dexamethasone or placebo on postoperative pain after single-visit root canal treatment in teeth with symptomatic irreversible pulpitis and symptomatic apical periodontitis.

    METHODOLOGY: The trial is reported according to the Preferred Reporting Items for RAndomized Trials in Endodontics (PRIRATE) 2020 guidelines. The protocol was registered at the clinical trial registry (India) (CTRI/2019/06/019818). In total, 160 patients, assigned to four groups, received orally either 20 mg piroxicam, 20 mg prednisolone, 4 mg dexamethasone or a placebo 60 min before root canal treatment. Patients recorded their postoperative pain intensity at 6, 12, 24, 48 and 72 h using a 10-cm visual analogue scale. Intergroup comparison was performed using Kruskal-Wallis tests with post hoc analysis using Dunns test. Incidence of pain was analysed using chi-square tests. A P value  0.05). One patient in the piroxicam group reported gastritis, whereas no adverse effects were recorded in other groups.

    CONCLUSION: Preoperative oral administration of a single dose of 4 mg dexamethasone, 20 mg piroxicam or 20 mg prednisolone reduced the incidence and severity of postoperative pain following single-visit root canal treatment compared to a placebo in patients with symptomatic irreversible pulpitis and symptomatic apical periodontitis up to 24 h. The odds of postoperative pain at 24 h for patients premedicated with 4 mg dexamethasone or 20 mg piroxicam or 20 mg prednisolone were 5.3 times, 3.4 times and 2.5 times less compared to the placebo, respectively.

    Matched MeSH terms: Administration, Oral
  4. Ibrahim AH, Khan MS, Al-Rawi SS, Ahamed MB, Majid AS, Al-Suede FS, et al.
    Regul Toxicol Pharmacol, 2016 Nov;81:457-467.
    PMID: 27756558 DOI: 10.1016/j.yrtph.2016.10.004
    Fermented Virgin Coconut Oil (FVCO) is widely used in the Southeast Asia as food and traditional medicine. The objective of the present study is the evaluation of chronic safety of the commercialized FVCO of Malaysia and other Southeast Asian countries. A single dose of 5000 mg/kg of FVCO was administered orally in rats (each group, n = 5) for the acute toxicity study and 175, 550 and 2000 mg/kg for sub-chronic and chronic studies (each group, n = 10), respectively. The behavior, mortality, and body weight of the rats were assessed to determine the toxic effects of FVCO. The haematology, biochemistry and histopathology of the treated rats were evaluated. The treated rats were safe with the dose of 5000 mg/kg in acute, sub-chronic and chronic indication. Abnormal clinical signs and morphology (gross necroscopy), changes of organ weight, anomalous haematology and biochemistry indexes were not found in comparison with the control (p > 0.05). In general, food and water intake were higher in the treated rats related to control. It was concluded that the presence of the antioxidant active compounds of FVCO might be the reason of safety. The structure activity relationship (SAR) provides a comprehensive mechanism to determine the safety that is the presence of the electron donating phenolic groups, carbonyl groups, and carboxylic acid in the ortho and meta position of the aromatic rings. The SAR showed the antioxidant properties of myristic acid and lauric acid determined by GC-MS analysis. This result suggests the safety of FVCO for chronic use, nutritional activity that FVCO formulation complies the requirements of regulatory agencies.
    Matched MeSH terms: Administration, Oral
  5. Thangavelu L, Balusamy SR, Shanmugam R, Sivanesan S, Devaraj E, Rajagopalan V, et al.
    Regul Toxicol Pharmacol, 2020 Jun;113:104640.
    PMID: 32169672 DOI: 10.1016/j.yrtph.2020.104640
    Acacia catechu (A. catechu) or Khair (Hindi) is used in several herbal preparations in the Ayurvedic system of medicine in India. Traditionally, this drug is beneficial against several gastrointestinal and stomach related ailments, and leprosy. The present investigation was carried out to evaluate the sub-acute oral toxicity of the ethanolic extract of A. catechu seeds in Wistar albino rats. Results obtained from the quantitative chemical analysis of A. catechu seed extract were compared with commercially available standards. A. catechu seed extract was administered orally at the doses of 250, 500 and 1000 mg/kg b.w. daily for 28 days. General behavior, bodyweight and mortality were examined during the entire study period. At the end of 28 days, hematological and biochemical parameters along with the relative organ weights were determined. It was observed that the extract did not induce death or any significant changes in the body weight, relative weight of vital organs and in hematological parameters for up to a dose of 1000 mg/kg. The oral administration of the plant extract did not produce any significant changes in the levels of glucose. In addition, there were no significant changes in the activity of both hepatotoxic and nephrotoxic marker enzymes in the serum. Oral administration of A. catechu also did not produce any significant changes in the levels of oxidative markers. Furthermore, the findings from the biochemical studies were, well corroborated with the histological findings.
    Matched MeSH terms: Administration, Oral
  6. Jaganathan SK, Vellayappan MV, Narasimhan G, Supriyanto E, Octorina Dewi DE, Narayanan AL, et al.
    World J Gastroenterol, 2014 Dec 7;20(45):17029-36.
    PMID: 25493015 DOI: 10.3748/wjg.v20.i45.17029
    Colon cancer arises due to the conversion of precancerous polyps (benign) found in the inner lining of the colon. Prevention is better than cure, and this is very true with respect to colon cancer. Various epidemiologic studies have linked colorectal cancer with food intake. Apple and berry juices are widely consumed among various ethnicities because of their nutritious values. In this review article, chemopreventive effects of these fruit juices against colon cancer are discussed. Studies dealing with bioavailability, in vitro and in vivo effects of apple and berry juices are emphasized in this article. A thorough literature survey indicated that various phenolic phytochemicals present in these fruit juices have the innate potential to inhibit colon cancer cell lines. This review proposes the need for more preclinical evidence for the effects of fruit juices against different colon cancer cells, and also strives to facilitate clinical studies using these juices in humans in large trials. The conclusion of the review is that these apple and berry juices will be possible candidates in the campaign against colon cancer.
    Matched MeSH terms: Administration, Oral
  7. Jaganathan SK, Vellayappan MV, Narasimhan G, Supriyanto E
    World J Gastroenterol, 2014 Apr 28;20(16):4618-25.
    PMID: 24782614 DOI: 10.3748/wjg.v20.i16.4618
    Colorectal cancer is the second leading cause of cancer-related deaths in the United States. Recent studies prove that though chemotherapeutic agents are being used for the treatment of colon cancer, they become non-effective when the cancer progresses to an invasive stage. Since consumption of certain dietary agents has been linked with various cancers, fruit juices have been investigated for their consistently protective effect against colon cancer. The unique biochemical composition of fruit juices is responsible for their anticancer properties. In this review, the chemo-preventive effect of fruit juices such as pomegranate and citrus juices against colon cancer are discussed. For this purpose, the bioavailability, in vitro and in vivo effects of these fruit juices on colorectal cancer are highlighted. Moreover, there is a scarcity of studies involving human trials to estimate the preventive nature of these juices against colon cancer. This review will support the need for more preclinical tests with these crude juices and their constituents in different colorectal cancer cell lines and also some epidemiological studies in order to have a better understanding and promote pomegranate and citrus juices as crusaders against colon cancer.
    Matched MeSH terms: Administration, Oral
  8. Xian TH, Sinniah K, Yean CY, Krishnamoorthy V, Bahari MB, Ravichandran M, et al.
    BMC Immunol, 2020 05 25;21(1):29.
    PMID: 32450807 DOI: 10.1186/s12865-020-00360-1
    BACKGROUND: Cholera, an acute watery diarrhoeal disease caused by Vibrio cholerae serogroup O1 and O139 across the continents. Replacing the existing WHO licensed killed multiple-dose oral cholera vaccines that demand 'cold chain supply' at 2-8 °C with a live, single-dose and cold chain-free vaccine would relieve the significant bottlenecks and cost determinants in cholera vaccination campaigns. In this direction, a prototype cold chain-free live attenuated cholera vaccine formulation (LACV) was developed against the toxigenic wild-type (WT) V. cholerae O139 serogroup. LACV was found stable and retained its viability (5 × 106 CFU/mL), purity and potency at room temperature (25 °C ± 2 °C, and 60% ± 5% relative humidity) for 140 days in contrast to all the existing WHO licensed cold-chain supply (2-8 °C) dependent killed oral cholera vaccines.

    RESULTS: The LACV was evaluated for its colonization potential, reactogenicity, immunogenicity and protective efficacy in animal models after its storage at room temperature for 140 days. In suckling mice colonization assay, the LACV recorded the highest recovery of (7.2 × 107 CFU/mL) compared to those of unformulated VCUSM14P (5.6 × 107 CFU/mL) and the WT O139 strain (3.5 × 107 CFU/mL). The LACV showed no reactogenicity even at an inoculation dose of 104-106 CFU/mL in a rabbit ileal loop model. The rabbits vaccinated with the LACV or unformulated VCUSM14P survived a challenge with WT O139 and showed no signs of diarrhoea or death in the reversible intestinal tie adult rabbit diarrhoea (RITARD) model. Vaccinated rabbits recorded a 275-fold increase in anti-CT IgG and a 15-fold increase in anti-CT IgA antibodies compared to those of rabbits vaccinated with unformulated VCUSM14P. Vibriocidal antibodies were increased by 31-fold with the LACV and 14-fold with unformulated VCUSM14P.

    CONCLUSION: The vaccine formulation mimics a natural infection, is non-reactogenic and highly immunogenic in vivo and protects animals from lethal wild-type V. cholerae O139 challenge. The single dose LACV formulation was found to be stable at room temperature (25 ± 2 °C) for 140 days and it would result in significant cost savings during mass cholera vaccination campaigns.

    Matched MeSH terms: Administration, Oral
  9. Wahab AA, Norliyana N, Ding CH, Nurzam SCH, Salbiah N, Rao KR
    Trop Biomed, 2020 Sep 01;37(3):560-565.
    PMID: 33612771 DOI: 10.47665/tb.37.3.560
    Primary prostatic melioidosis is a rare presentation of melioidosis even in melioidosis endemic areas. We report a case of a 58-year-old man with underlying diabetes mellitus who presented with a 5-day history of high-grade fever associated with lower urinary tract symptoms. Suprapubic tenderness and tender prostatomegaly were noted on examination. An abdominal computed tomography (CT) scan confirmed the presence of a prostatic abscess. Both blood and prostatic pus cultures grew Burkholderia pseudomallei. He was initially started on intravenous ceftazidime, followed by an escalation to intravenous meropenem. He was discharged home with oral amoxicillin-clavulanate and doxycycline after completing 12 days of meropenem. Unfortunately, his compliance to oral antibiotic therapy was poor, and he succumbed to the disease.
    Matched MeSH terms: Administration, Oral
  10. 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: Administration, Oral
  11. Akram Z, Abduljabbar T, Kellesarian SV, Abu Hassan MI, Javed F, Vohra F
    Br J Clin Pharmacol, 2017 03;83(3):444-454.
    PMID: 27718252 DOI: 10.1111/bcp.13147
    AIMS: The aim of this systematic review was to assess the efficacy of bisphosphonate therapy as an adjunct to scaling and root planing (SRP) in the management of periodontitis.

    METHODS: Databases (MEDLINE, EMBASE, Cochrane Central Register of Controlled Trials and Cochrane Oral Health Group Trials Register databases) were searched up to and including July 2016. The primary outcome was probing depth (PD), and the secondary outcomes were changes in clinical attachment level (CAL) and bone defect (BD) fill. The mean differences (MD) of outcomes and 95% confidence intervals (CI) for each variable were calculated using random effect model.

    RESULTS: Eight clinical studies were included. Seven studies used alendronate as an adjunct to SRP; of these, four studies used topical application and three used oral alendronate. Considering the effects of adjunctive bisphosphonates as compared to SRP alone, a high degree of heterogeneity for PD (Q value = 39.6, P 

    Matched MeSH terms: Administration, Oral
  12. Mordi MN, Mansor SM, Navaratnam V, Wernsdorfer WH
    Br J Clin Pharmacol, 1997 Apr;43(4):363-5.
    PMID: 9146847
    AIMS: To determine the pharmacokinetics of artemether (ARM) and its principal active metabolite, dihydroartemisinin (DHA) in healthy volunteers.

    METHODS: Six healthy male Malaysian subjects were given a single oral dose of 200 mg artemether. Blood samples were collected to 72 h. Plasma concentrations of the two compounds were measured simultaneously by reversed-phase h.p.l.c. with electro-chemical detection in the reductive mode.

    RESULTS: Mean (+/- s.d.) maximum concentrations of ARM, 310 +/- 153 micrograms l-1, were reached 1.88 +/- 0.21 h after drug intake. The mean elimination half-life was 2.00 +/- 0.59 h, and the mean AUC 671 +/- 271 micrograms l-1 h. The mean Cmax of DHA, 273 +/- 64 micrograms l-1 was observed at 1.92 +/- 0.13 h. The mean AUC of DHA was 753 +/- 233 micrograms h l-1'. ARM and DHA were stable at < or = -20 degrees C for at least 4 months in plasma samples.

    CONCLUSIONS: The relatively short half-life of ARM may be one of the factors responsible for the poor radical cure rate of falciparum malaria with regimens employing daily dosing. In view of the rapid loss of DHA in plasma samples held at room temperature (26 degrees C) it is recommended to store them at a temperature of < or = -20 degrees C as early as possible after sample collection.

    Matched MeSH terms: Administration, Oral
  13. Nyam KL, Chang CY, Tan CS, Ng ST
    Int J Med Mushrooms, 2016;18(12):1093-1104.
    PMID: 28094747 DOI: 10.1615/IntJMedMushrooms.v18.i12.40
    The aim of this study was to determine the antiulcer activity of Lignosus rhinocerotis in rats. A total of 48 Sprague-Dawley rats were used in ethanol-induced, aspirin-induced, and water immersion-restraint stress-induced ulcer models. Rats were equally divided into 4 groups for each model and orally administered 5 mL/kg distilled water, 20 mg/kg omeprazole, as well as 250 and 500 mg/kg of L. rhinocerotis powder. L. rhinocerotis powder at both 250 and 500 mg/kg doses demonstrated significant (P < 0.05) protection against gastric ulceration in all the induced ulcer models. Histological studies revealed severe damage and hemorrhage of gastric mucosa in the negative control group for all ulcer-induced models. The study suggests that L. rhinocerotis powder possesses dose-dependent antiulcer activity in the gastric mucosa, as ascertained grossly and histologically, compared with the negative control groups.
    Matched MeSH terms: Administration, Oral
  14. Rahman H, Pradhan A, Kharka L, Renjhen P, Kar S, Dutta S
    J Obstet Gynaecol Can, 2013 May;35(5):408-416.
    PMID: 23756271 DOI: 10.1016/S1701-2163(15)30931-2
    OBJECTIVES: To assess and compare the efficacy and safety of 50 µg oral misoprostol and 25 µg intravaginal misoprostol for induction of labour at term.

    METHODS: This non-blinded, randomized clinical trial included 228 pregnant women at term with obstetric or medical indications for induction of labour. Women either took 50 µg misoprostol orally (two 25 µg tablets) or had one 25 µg tablet of misoprostol inserted in the posterior vaginal fornix. In each group, misoprostol administration was repeated every four hours in the same dose until regular uterine contractions were established or to a maximum of five doses. Time to delivery and outcome data for each group were compared.

    RESULTS: Of the 228 women, eight (3.5%) were excluded from the analysis as they withdrew their consent after randomization. Mean induction-to-delivery interval was similar in both groups (21.22 hours in the oral group vs. 20.15 hours in the vaginal group; P = 0.58). There was no significant difference between the groups with respect to the number of women who delivered within 24 hours or who required oxytocin augmentation of labour, the mode of delivery, and neonatal outcomes (P > 0.05). Uterine hyperstimulation occurred in two women who received misoprostol vaginally, but not in any of the women in the oral misoprostol group.

    CONCLUSION: Oral misoprostol in a dose of 50 µg every four hours, to a maximum of five doses, has the potential to induce labour as safely and effectively as 25 µg misoprostol administered vaginally every four hours.

    Matched MeSH terms: Administration, Oral
  15. Tan TW, Chen BC, Tan HL, Chang CM
    JBI Database System Rev Implement Rep, 2017 Apr;15(4):862-872.
    PMID: 28398972 DOI: 10.11124/JBISRIR-2016-003034
    REVIEW QUESTION/OBJECTIVE: This review aims to determine the best available evidence related to the effectiveness of amylmetacresol and 2,4-dichlorobenzyl alcohol throat lozenges in patients with acute sore throat due to upper respiratory tract infection (URTI). The objective is to examine the analgesic properties of amylmetacresol and 2,4-dichlorobenzyl alcohol (AMC/DCBA) throat lozenge comparing with placebo for the relief of pain in patients with acute sore throat due to URTIs.The review question is:More specifically, the objectives are to.
    Matched MeSH terms: Administration, Oral
  16. Adeeb N, Fong TN
    Med J Malaysia, 1974 Jun;28(4):263-6.
    PMID: 4278401
    Matched MeSH terms: Administration, Oral
  17. Leong LL
    Med J Malaysia, 1976 Mar;30(3):229-37.
    PMID: 1085401
    Matched MeSH terms: Administration, Oral
  18. Chung ELT, Predith M, Nobilly F, Samsudin AA, Jesse FFA, Loh TC
    Trop Anim Health Prod, 2018 Jun 20.
    PMID: 29926360 DOI: 10.1007/s11250-018-1641-4
    Brachiaria decumbens is an extremely productive tropical grass due to its aggressive growth habit and its adaptation to a varied range of soil types and environments. As a result of the vast availability, treated B. decumbens demonstrates as a promising local material that could be utilised as an improved diet for sheep and goats. Despite the fact that the grass significantly increases weight gains in grazing farm animals, there were many reports of general ill-thrift and sporadic outbreaks of photosensitivity in livestock due to the toxic compound of steroidal saponin found in B. decumbens. Ensiling and haymaking were found to be effective in removing toxin and undesirable compounds in the grass. Biological treatments using urea, activated charcoal, polyethylene glycol, and effective microorganisms were found to be useful in anti-nutritional factor deactivation and improving the nutritive values of feedstuffs. Besides, oral administration of phenobarbitone showed some degree of protection in sheep that fed on B. decumbens pasture. In this review, we aim to determine the effect of B. decumbens toxicity and possible treatment methods on the grass to be used as an improved diet for small ruminant.
    Matched MeSH terms: Administration, Oral
  19. Auwal SM, Zarei M, Tan CP, Basri M, Saari N
    Sci Rep, 2018 Jul 10;8(1):10411.
    PMID: 29991723 DOI: 10.1038/s41598-018-28659-5
    Bromelain-generated biopeptides from stone fish protein exhibit strong inhibitory effect against ACE and can potentially serve as designer food (DF) with blood pressure lowering effect. Contextually, the DF refer to the biopeptides specifically produced to act as ACE-inhibitors other than their primary role in nutrition and can be used in the management of hypertension. However, the biopeptides are unstable under gastrointestinal tract (GIT) digestion and need to be stabilized for effective oral administration. In the present study, the stone fish biopeptides (SBs) were stabilized by their encapsulation in sodium tripolyphosphate (TPP) cross-linked chitosan nanoparticles produced by ionotropic gelation method. The nanoparticles formulation was then optimized via Box-Behnken experimental design to achieve smaller particle size (162.70 nm) and high encapsulation efficiency (75.36%) under the optimum condition of SBs:Chitosan mass ratio (0.35), homogenization speed (8000 rpm) and homogenization time (30 min). The SBs-loaded nanoparticles were characterized for morphology by transmission electron microscopy (TEM), physicochemical stability and efficacy. The nanoparticles were then lyophilized and analyzed using Fourier transform infra-red spectroscopy (FTIR) and X-ray diffraction (XRD). The results obtained indicated a sustained in vitro release and enhanced physicochemical stability of the SBs-loaded nanoparticles with smaller particle size and high encapsulation efficiency following long period of storage. Moreover, the efficacy study revealed improved inhibitory effect of the encapsulated SBs against ACE following simulated GIT digestion.
    Matched MeSH terms: Administration, Oral
  20. Ling Tan JS, Roberts CJ, Billa N
    Pharm Dev Technol, 2019 Apr;24(4):504-512.
    PMID: 30132723 DOI: 10.1080/10837450.2018.1515225
    This study describes the properties of an amphotericin B-containing mucoadhesive nanostructured lipid carrier (NLC), with the intent to maximize uptake within the gastrointestinal tract. We have reported previously that lipid nanoparticles can significantly improve the oral bioavailability of amphotericin B (AmpB). On the other hand, the aggregation state of AmpB within the NLC has been ascribed to some of the side effects resulting from IV administration. In the undissolved state, AmpB (UAmpB) exhibited the safer monomeric conformation in contrast to AmpB in the dissolved state (DAmpB), which was aggregated. Chitosan-coated NLC (ChiAmpB NLC) presented a slightly slower AmpB release profile as compared to the uncoated formulation, achieving 26.1% release in 5 hours. Furthermore, the ChiAmpB NLC formulation appeared to prevent the expulsion of AmpB upon exposure to simulated gastrointestinal pH media, whereby up to 63.9% of AmpB was retained in the NLC compared to 56.1% in the uncoated formulation. The ChiAmpB NLC demonstrated mucoadhesive properties in pH 5.8 and 6.8. Thus, the ChiAmpB NLC formulation is well-primed for pharmacokinetic studies to investigate whether delayed gastrointestinal transit may be exploited to improve the systemic bioavailability of AmpB, whilst simultaneously addressing the side-effect concerns of AmpB.
    Matched MeSH terms: Administration, Oral
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