Displaying publications 41 - 60 of 64 in total

Abstract:
Sort:
  1. Nawaz MS, Shah KU, Khan TM, Rehman AU, Rashid HU, Mahmood S, et al.
    Diabetes Metab Syndr, 2017 Dec;11 Suppl 2:S833-S839.
    PMID: 28709853 DOI: 10.1016/j.dsx.2017.07.003
    OBJECTIVE: Diabetes mellitus is a major health problem in developing countries. There are various insulin therapies to manage diabetes mellitus. This systematic review evaluates various insulin therapies for management of diabetes mellitus worldwide. This review also focuses on recent developments being explored for better management of diabetes mellitus.

    RESEARCH DESIGN AND METHOD: We reviewed a number of published articles from 2002 to 2016 to find out the appropriate management of diabetes mellitus. The paramount parameters of the selected studies include the insulin type & its dose, type of diabetes, duration and comparison of different insulin protocols. In addition, various newly developed approaches for insulin delivery with potential output have also been evaluated.

    RESULTS: A great variability was observed in managing diabetes mellitus through insulin therapy and the important controlling factors found for this therapy include; dose titration, duration of insulin use, type of insulin used and combination therapy of different insulin.

    CONCLUSION: A range of research articles on current trends and recent advances in insulin has been summarized, which led us to the conclusion that multiple daily insulin injections or continuous subcutaneous insulin infusion (insulin pump) is the best method to manage diabetes mellitus. In future perspectives, development of the oral and inhalant insulin would be a tremendous breakthrough in Insulin therapy.

    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  2. Ngo YL, Lau CH, Chua LS
    Food Chem Toxicol, 2018 Nov;121:687-700.
    PMID: 30273632 DOI: 10.1016/j.fct.2018.09.064
    Rosmarinic acid is a bioactive phytochemical that can be found in many herbs as ethnomedicines. It possesses remarkable pharmacological activities, and thus leading to its exploration as a therapeutic drug in diabetes treatment recently. This article reviews the extraction and fractionation techniques for plant-based natural rosmarinic acid and its anti-diabetic potential based on literature data published in journals, books, and patents from 1958 to 2017. Factors affecting the performance of rosmarinic acid extraction and fractionation such as operating temperature, time, solvent to sample ratio and eluent system are compiled and discussed in detail. The inhibitory action of rosmarinic acid against sugar digestive enzymes, and protective action towards pancreatic β-cell dysfunction and glucolipotoxicity mediated oxidative stress are also critically reviewed. The optimal parameters are largely dependent on the applied extraction and fractionation techniques, as well as the nature of plant samples. Previous studies have proven the potent role of rosmarinic acid to control plasma glucose level and increase insulin sensitivity in hyperglycemia. Although rosmarinic acid is readily absorbed by human body, its mechanism after consumption is remained unclear. Intensive studies should be well planned to determine the dosage and toxicity level of rosmarinic acid for efficacy and safe consumption.
    Matched MeSH terms: Diabetes Mellitus/drug therapy
  3. Rasouli M, Ahmad Z, Omar AR, Allaudin ZN
    BMC Biotechnol, 2011 Nov 03;11:99.
    PMID: 22047106 DOI: 10.1186/1472-6750-11-99
    BACKGROUND: Diabetes mellitus is a complicated disease with a pathophysiology that includes hyperinsulinemia, hyperglycemia and other metabolic impairments leading to many clinical complications. It is necessary to develop appropriate treatments to manage the disease and reduce possible acute and chronic side effects. The advent of gene therapy has generated excitement in the medical world for the possible application of gene therapy in the treatment of diabetes. The glucagon-like peptide-1 (GLP-1) promoter, which is recognised by gut L-cells, is an appealing candidate for gene therapy purposes. The specific properties of L-cells suggest that L-cells and the GLP-1 promoter would be useful for diabetes therapy approaches.

    RESULTS: In this study, L-cells were isolated from a primary intestinal cell line to create suitable target cells for insulin expression studies. The isolated cells displayed L-cell properties and were therefore used as an L-cell surrogate. Next, the isolated L-cells were transfected with the recombinant plasmid consisting of an insulin gene located downstream of the GLP-1 promoter. The secretion tests revealed that an increase in glucose concentration from 5 mM to 25 mM induced insulin gene expression in the L-cells by 2.7-fold. Furthermore, L-cells quickly responded to the glucose stimulation; the amount of insulin protein increased 2-fold in the first 30 minutes and then reached a plateau after 90 minutes.

    CONCLUSION: Our data showed that L-cells efficiently produced the mature insulin protein. In addition, the insulin protein secretion was positively regulated with glucose induction. In conclusion, GLP-1 promoter and L-cell could be potential candidates for diabetes gene therapy agents.

    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  4. Rozman NAS, Tong WY, Leong CR, Anuar MR, Karim S, Ong SK, et al.
    Sci Rep, 2020 02 24;10(1):3307.
    PMID: 32094395 DOI: 10.1038/s41598-020-60364-0
    Essential oil of Homalomena pineodora inhibits diabetic pathogens; however, the activity was not sustainable when applied as wound dressing. This study aims to synthesise the essential oil nanoparticle using chitosan. The nanoparticles were synthesised with ion gelation method, confirmed by spectroscopic analysis. The spherical nanoparticles display a size of 70 nm, with strong surface charge of +24.10 mV. The nanoparticles showed an initial burst release followed by a slow release pattern for 72 h, following the first order of kinetic. The release behaviour was ideal for wound dressing. The antimicrobial activity was broad spectrum. The formation of nanoparticle enhanced the antimicrobial efficacy of the essential oil. The nanoparticle also showed a concentration-dependent killing behaviour on time-kill assay. In the 3D collagen wound models, the nanoparticles reduced the microbial growth by 60-80%. In conclusion, H. pineodora nanoparticles showed pharmaceutical potential in inhibiting microbial growth on diabetic ulcers.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  5. Saddique FA, Aslam S, Ahmad M, Ashfaq UA, Muddassar M, Sultan S, et al.
    Molecules, 2021 May 20;26(10).
    PMID: 34065194 DOI: 10.3390/molecules26103043
    Diabetes mellitus (DM) is a chronic disorder and has affected a large number of people worldwide. Insufficient insulin production causes an increase in blood glucose level that results in DM. To lower the blood glucose level, various drugs are employed that block the activity of the α-glucosidase enzyme, which is considered responsible for the breakdown of polysaccharides into monosaccharides leading to an increase in the intestinal blood glucose level. We have synthesized novel 2-(3-(benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl)-N-arylacetamides and have screened them for their in silico and in vitro α-glucosidase inhibition activity. The derivatives 11c, 12a, 12d, 12e, and 12g emerged as potent inhibitors of the α-glucosidase enzyme. These compounds exhibited good docking scores and excellent binding interactions with the selected residues (Asp203, Asp542, Asp327, His600, Arg526) during in silico screening. Similarly, these compounds also showed good in vitro α-glucosidase inhibitions with IC50 values of 30.65, 18.25, 20.76, 35.14, and 24.24 μM, respectively, which were better than the standard drug, acarbose (IC50 = 58.8 μM). Furthermore, a good agreement was observed between in silico and in vitro modes of study.
    Matched MeSH terms: Diabetes Mellitus/drug therapy
  6. Sah SK, Samuel VP, Dahiya S, Singh Y, Gilhotra RM, Gupta G, et al.
    Chem Biol Interact, 2019 Jun 01;306:117-122.
    PMID: 31004596 DOI: 10.1016/j.cbi.2019.04.022
    Major challenges of dealing elder patients with diabetes mellitus (DM) are the individualization of consideration in persons with various comorbid types of conditions. In spite of the fact that microvascular and macrovascular problems associated with DM are well documented, there is only a few numbers of reports viewing different conditions, for example, cognitive dysfunction. Cognitive dysfunction is of specific significance due to its effect on self-care and quality of life. All in all, the etiology of cognitive dysfunction in the maturing populace is probably going to be the grouping of ischemic and degenerative pathology. It is likewise trusted that Hyperglycemia is engaged with the system of DM-related cognitive dysfunction. At present, it isn't certain in the case of enhancing glycemic control or utilizing therapeutic agents can enhance the risk of cognitive decay. Amylin was later characterized as an amyloidogenic peptide, confined from a beta cell tumor and called islet amyloid polypeptide (IAPP), and after that, amylin. Conversely, we investigate the beneficial role and hypothesizing the mechanism of amylin related expanding the level and activation of CGRP receptor to enhance the cognition declination amid diabetic dementia.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  7. Sengupta P, Chatterjee B, Pal TK
    Regul Toxicol Pharmacol, 2017 Dec;91:151-158.
    PMID: 29107617 DOI: 10.1016/j.yrtph.2017.10.029
    The prevalence of hypertension is very common amongst the diabetic patients and is reported as the major cause of mortality in diabetes. Pioglitazone reported to have an ability to alter the blood cholesterol level and cardioprotective efficiency along with its antidiabetic activity. Telmisartan, through activation of PPAR-γ receptor exerts insulin sensitizing property in addition to its primary cardioprotective efficiency. Theoretically, a combination of pioglitazone and telmisartan may be beneficial to effectively control the high blood glucose level and management of coexisting cardiovascular complication in diabetes. The aim of this research was to experimentally evaluate the pharmacokinetic interaction of pioglitazone and telmisartan when are coadministered in rat. Pioglitazone and telmisartan were administered orally as a single dose individually and in combination to the rats. The plasma samples of the pharmacokinetic study were analyzed using a validated LCMS method. The acute toxicity of the combination with a high dose in rats was also evaluated as a part of the determination of its safety profile. There was no significant change in pharmacokinetic parameters were resulted due to the coadministration of pioglitazone and telmisartan in rat. Absence of major toxicological effect supports the in vivosafety of the combination.
    Matched MeSH terms: Diabetes Mellitus/drug therapy
  8. Shahcheraghi SH, Aljabali AAA, Al Zoubi MS, Mishra V, Charbe NB, Haggag YA, et al.
    Life Sci, 2021 Aug 01;278:119632.
    PMID: 34019900 DOI: 10.1016/j.lfs.2021.119632
    Diabetes epidemiological quantities are demonstrating one of the most important communities' health worries. The essential diabetic difficulties are including cardiomyopathy, nephropathy, inflammation, and retinopathy. Despite developments in glucose decreasing treatments and drugs, these diabetic complications are still ineffectively reversed or prohibited. Several signaling and molecular pathways are vital targets in the new therapies of diabetes. This review assesses the newest researches about the key molecules and signaling pathways as targets of molecular pharmacology in diabetes and diseases related to it for better treatment based on molecular sciences. The disease is not cured by current pharmacological strategies for type 2 diabetes. While several drug combinations are accessible that can efficiently modulate glycemia and mitigate long-term complications, these agents do not reverse pathogenesis, and in practice, they are not established to modify the patient's specific molecular profiling. Therapeutic companies have benefited from human genetics. Genome exploration, which is agnostic to the information that exists, has revealed tens of loci that impact glycemic modulation. The physiological report has begun to examine subtypes of diseases, illustrate heterogeneity and propose biochemical therapeutic pathways.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  9. Solayman M, Ali Y, Alam F, Islam MA, Alam N, Khalil MI, et al.
    Curr Pharm Des, 2016;22(5):549-65.
    PMID: 26601968
    Diabetes mellitus (DM) is one of the most common endocrine metabolic disorders. In addition to exercise and diet, oral anti-diabetic drugs have been used as a part of the management strategy worldwide. Unfortunately, none of the conventional anti-diabetic drugs are without side effects, and these drugs pose an economic burden. Therefore, the investigation of novel anti-diabetic regimens is a major challenge for researchers, in which nature has been the primary resource for the discovery of potential therapeutics. Many plants have been shown to act as anti-diabetic agents, in which the main active constituents are believed to be polyphenols. Natural products containing high polyphenol levels can control carbohydrate metabolism by various mechanisms, such as protecting and restoring beta-cell integrity, enhancing insulin releasing activity, and increasing cellular glucose uptake. Blackberries, red grapes, apricots, eggplant and popular drinks such as coffee, cocoa and green tea are all rich in polyphenols, which may dampen insulin resistance and be natural alternatives in the treatment of diabetes. Therefore, the aim of this review is to report on the available anti-diabetic polyphenols (medicinal plants, fruits and vegetables), their mechanisms in the various pathways of DM and their correlations with DM. Additionally, this review emphasizes the types of polyphenols that could be potential future resources in the treatment of DM via either novel regimens or as supplementary agents.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  10. Taha M, Sultan S, Imran S, Rahim F, Zaman K, Wadood A, et al.
    Bioorg Med Chem, 2019 09 15;27(18):4081-4088.
    PMID: 31378594 DOI: 10.1016/j.bmc.2019.07.035
    In searchof the potenttherapeutic agent as an α-glucosidase inhibitor, we have synthesized twenty-five analogs (1-25) of quinoline-based Schiff bases as an inhibitoragainst α-glucosidase enzyme under positive control acarbose (IC50 = 38.45 ± 0.80 µM). From the activity profile it was foundthat analogs 1, 2, 3, 4, 11, 12 and 20with IC50values 12.40 ± 0.40, 9.40 ± 0.30, 14.10 ± 0.40, 6.20 ± 0.30, 14.40 ± 0.40, 7.40 ± 0.20 and 13.20 ± 0.40 µMrespectively showed most potent inhibition among the series even than standard drug acarbose (IC50 = 38.45 ± 0.80 µM). Here in the present study analog 4 (IC50 = 6.20 ± 0.30 µM) was found with many folds better α-glucosidase inhibitory activity than the reference drug. Eight analogs like 5, 7, 8, 16, 17, 22, 24 and 25 among the whole series displayed less than 50% inhibition. The substituents effects on phenyl ring thereby superficially established through SAR study. Binding interactions of analogs and the active site of ligands proteins were confirmed through molecular docking study. Spectroscopic techniques like 1H NMR, 13C NMR and ESIMS were used for characterization.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  11. Tang KS
    Life Sci, 2019 Dec 15;239:117011.
    PMID: 31669241 DOI: 10.1016/j.lfs.2019.117011
    Diabetes mellitus (DM) is a multifaceted and costly disease, which requires serious attention. Finding a cheaper anti-diabetic alternative that can act on multiple disease-related targets and pathways is the ultimate treatment goal for DM. Nanotechnology has offered some exciting possibilities in biomedical and drug delivery applications. Zinc oxide nanoparticles (ZnO-NPs), a novel agent to deliver zinc, have great implications in many disease therapies including DM. This review summarizes the pharmacological mechanisms by which ZnO-NPs alleviate DM and diabetic complications. Research implications and future perspectives were also discussed.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  12. Thent ZC, Das S, Zaidun NH
    Curr Drug Deliv, 2018;15(4):453-460.
    PMID: 28545355 DOI: 10.2174/1567201814666170525122224
    BACKGROUND: The incidence of diabetes mellitus has increased drastically over the past few decades. This oxidant-antioxidant imbalance resulting in complication of diabetes mellitus includes macro- and microvascular complications. Resistance to conventional treatment and patient compliance has paved the way to the usage of effective natural products and supplements. Momordica charantia (bitter gourd) is widely consumed in many parts of Malaysia as a vegetable. Momordica charantia (MC) is mainly used in the management of diabetes mellitus.

    OBJECTIVE: The present review discusses the literature concerning the antidiabetic and antioxidant properties of MC focusing on the complication of diabetes mellitus along with its mode of delivery. We found that among the whole part of MC, its fruit extract has been widely studied, therapeutically. The evidence based analysis of the beneficiary effects of MC on the different organs involved in diabetes complication is also highlighted. This review elucidated an essential understanding of MC based drug delivery system in both clinical and experimental studies and appraised the great potential of the protein based MC extract against diabetes mellitus.

    CONCLUSION: The review paper is believed to assist the researchers and medical personnel in treating diabetic associated complications.

    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  13. Thomas A, Rajesh EK, Kumar DS
    Phytother Res, 2016 Mar;30(3):357-66.
    PMID: 26749336 DOI: 10.1002/ptr.5559
    Tinospora crispa is a medicinal plant belonging to the botanical family Menispermiaceae. The plant is widely distributed in Southeast Asia and the northeastern region of India. A related species Tinospora cordifolia is used in Ayurveda for treating a large spectrum of diseases. Traditional healers of Thailand, Malaysia, Guyana, Bangladesh and the southern Indian province of Kerala use this plant in the treatment of diabetes. Many diterpenes, triterpenes, phytosteroids, alkaloids and their glycosides have been isolated from T. crispa. Cell culture and animal studies suggest that the herb stimulates secretion of insulin from β-cells. It also causes dose-dependent and time-dependent enhancement of glucose uptake in muscles. However, in view of the reported hepatotoxicity, this herb may be used with caution. This article reviews the animal studies and human clinical trials carried out using this herb. Areas of future research are also identified.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  14. Tiong SH, Looi CY, Hazni H, Arya A, Paydar M, Wong WF, et al.
    Molecules, 2013 Aug 15;18(8):9770-84.
    PMID: 23955322 DOI: 10.3390/molecules18089770
    Catharanthus roseus (L.) G. Don is a herbal plant traditionally used by local populations in India, South Africa, China and Malaysia to treat diabetes. The present study reports the in vitro antioxidant and antidiabetic activities of the major alkaloids isolated from Catharanthus roseus (L.) G. Don leaves extract. Four alkaloids--vindoline I, vindolidine II, vindolicine III and vindolinine IV--were isolated and identified from the dichloromethane extract (DE) of this plant's leaves. DE and compounds I-III were not cytotoxic towards pancreatic β-TC6 cells at the highest dosage tested (25.0 µg/mL). All four alkaloids induced relatively high glucose uptake in pancreatic β-TC6 or myoblast C2C12 cells, with III showing the highest activity. In addition, compounds II-IV demonstrated good protein tyrosine phosphatase-1B (PTP-1B) inhibition activity, implying their therapeutic potential against type 2 diabetes. III showed the highest antioxidant potential in ORAC and DPPH assays and it also alleviated H₂O₂-induced oxidative damage in β-TC6 cells at 12.5 µg/mL and 25.0 µg/mL.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  15. Tong WT, Lee YK, Ng CJ, Lee PY
    PLoS One, 2020;15(12):e0244645.
    PMID: 33378349 DOI: 10.1371/journal.pone.0244645
    BACKGROUND: Many patient decision aids (PDAs) are developed in academic settings by academic researchers. Academic settings are different from public health clinics where the focus is on clinical work. Thus, research on implementation in public health settings will provide insights to effective implementation of PDA in real-world settings. This study explores perceived factors influencing implementation of an insulin PDA in five public health clinics.

    METHODS: This study adopted a comparative case study design with a qualitative focus to identify similarities and differences of the potential barriers and facilitators to implementing the insulin PDA across different sites. Focus groups and individual interviews were conducted with 28 healthcare providers and 15 patients from five public health clinics under the Ministry of Health in Malaysia. The interviews were transcribed verbatim and analysed using the thematic approach.

    RESULTS: Five themes emerged which were: 1) time constraint; 2) PDA costs; 3) tailoring PDA use to patient profile; 4) patient decisional role; and 5) leadership and staff motivation. Based on the interviews and drawing on observations and interview reflection notes, time constraint emerged as the common prominent factor that cut across all the clinics, however, tailoring PDA use to patient profile; patient decisional role; leadership and staff motivation varied due to the distinct challenges faced by specific clinics. Among clinics from semi-urban areas with more patients from limited education and lower socio-economic status, patients' ability to comprehend the insulin PDA and their tendency to rely on their doctors and family to make health decisions were felt to be a prominent barrier to the insulin PDA implementation. Staff motivation appeared to be stronger in most of the clinics where specific time was allocated to diabetes team to attend to diabetes patients and this was felt could be a potential facilitator, however, a lack of leadership might affect the insulin PDA implementation even though a diabetes team is present.

    CONCLUSIONS: This study found time constraint as a major potential barrier for PDA implementation and effective implementation of the insulin PDA across different public health clinics would depend on leadership and staff motivation and, the need to tailor PDA use to patient profile. To ensure successful implementation, implementers should avoid a 'one size fits all' approach when implementing health innovations.

    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  16. Tong WT, Lee YK, Ng CJ, Lee PY
    Implement Sci, 2017 03 21;12(1):40.
    PMID: 28327157 DOI: 10.1186/s13012-017-0569-9
    BACKGROUND: Most studies on barriers and facilitators to implementation of patient decision aids (PDAs) are conducted in the west; hence, the findings may not be transferable to developing countries. This study aims to use a locally developed insulin PDA as an exemplar to explore the barriers and facilitators to implementing PDAs in Malaysia, an upper middle-income country in Asia.
    METHODS: Qualitative methodology was adopted. Nine in-depth interviews (IDIs) and three focus group discussions (FGDs) were conducted with policymakers (n = 6), medical officers (n = 13), diabetes educators (n = 5) and a nurse, who were involved in insulin initiation management at an academic primary care clinic. The interviews were conducted with the aid of a semi-structured interview guide based on the Theoretical Domains Framework. The interviews were audio-recorded, transcribed verbatim and analyzed using a thematic approach.
    RESULTS: Five themes emerged, and they were lack of shared decision-making (SDM) culture, role boundary, lack of continuity of care, impact on consultation time and reminder network. Healthcare providers' (HCPs) paternalistic attitude, patients' passivity and patient trust in physicians rendered SDM challenging which affected the implementation of the PDA. Clear role boundaries between the doctors and nurses made collaborative implementation of the PDA challenging, as nurses may not view the use of insulin PDA to be part of their job scope. The lack of continuity of care might cause difficulties for doctors to follow up on insulin PDA use with their patient. While time was the most commonly cited barrier for PDA implementation, use of the PDA might reduce consultation time. A reminder network was suggested to address the issue of forgetfulness as well as to trigger interest in using the PDA. The suggested reminders were peer reminders (i.e. HCPs reminding one another to use the PDA) and system reminders (e.g. incorporating electronic medical record prompts, displaying posters/notices, making the insulin PDA available and visible in the consultation rooms).
    CONCLUSIONS: When implementing PDAs, it is crucial to consider the healthcare culture and system, particularly in developing countries such as Malaysia where concepts of SDM and PDAs are still novel.
    Study site: primary care clinic, University Malaya Medical Centre (UMMC), Kuala Lumpur, Malaysia
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  17. Wong TW
    J Drug Target, 2010 Feb;18(2):79-92.
    PMID: 19968567 DOI: 10.3109/10611860903302815
    The possibility of administering insulin orally in replacement of painful subcutaneous route has been investigated over years but with varying degree of success. Nanoparticles, microparticles, hydrogel, capsule, tablet, and film patch are designed to deliver insulin orally. They are largely formulated with polymeric adhesive, protease inhibitor, insulin aggregation inhibitor, and functional excipients to induce transcellular, paracellular, Peyer's patches, or receptor-mediated transport of insulin in gastrointestinal tract. Superporous matrix, intestinal patches, and charged-coupled micromagnet microparticles are recent formulation strategies to promote oral insulin absorption. The formulation emphasizes on assembly of insulin and excipients into a physical structure which provides an element of drug targeting to maintain stability and increase bioavailability of insulin. The overview of various strategies applied in oral insulin delivery system design denotes the significance of mucoadhesiveness whereby a prolonged retention of dosage form in intestinal tract translates to cumulative insulin release and absorption, overcoming the intestinal transport capacity limit. Synthesis and use of mucoadhesive excipients, chemical modification of insulin to promote its physicochemical and biological stability for encapsulation in dosage form with prolonged retention characteristics and identification of potential insulin adjuncts are efforts needed to accelerate the speed of obtaining a functional oral insulin delivery system.
    Matched MeSH terms: Diabetes Mellitus/drug therapy*
  18. Wong TW
    Recent Pat Drug Deliv Formul, 2009 Jan;3(1):8-25.
    PMID: 19149726 DOI: 10.2174/187221109787158346
    The global burden of diabetes is estimated to escalate from about 171 million in 2000 to 366 million people in 2030. The routine of diabetes treatment by injection of insulin incurs pain and has been one major factor negating the quality of life of diabetic patients. The possibility of administering insulin via alternative routes such as oral and nasal pathways has been investigated over the years, but with insulin experiencing risks of enzymatic degradation and poor transmucosal absorption. This leads to the rising needs to develop new formulation strategies emphasizing on the assembly of insulin and excipients into a physical structure to maintain the stability and increase the bioavailability of insulin. Chitosan and its derivatives or salts have been widely investigated as functional excipients of delivering insulin via oral, nasal and transdermal routes. The overview of various recent patented strategies on non-injection insulin delivery denotes the significance of chitosan for its mucoadhesive and able to protect the insulin from enzymatic degradation, prolong the retention time of insulin, as well as, open the inter-epithelial tight junction to facilitate systemic insulin transport. The chitosan can be employed to strengthen the physicochemical stability of insulin and multi-particulate matrix. The introduction of chitosan coat or co-formulation of chitosan with cationic gelatin or electrolytes which provide solidified or partially crosslinked structures retain and/or enhance the positive charges of dosage form necessary to induce mucoadhesiveness. The chitosan is modifiable chemically to produce water-soluble low molecular weight polymer which renders insulin able to be processed under mild conditions, and sulphated chitosan which markedly opens the paracellular channels for insulin transport. Combination of chitosan and fatty acid as hydrophobic nanoparticles promotes the insulin absorption via lymphoid tissue. Attainment of optimized formulations with higher levels of pharmacological bioavailability is deemed possible in future through targeted delivery of insulin using chitosan with specific adhesiveness to the intended absorption mucosa.
    Matched MeSH terms: Diabetes Mellitus/drug therapy
  19. Wong TW, Sumiran N
    J Pharm Pharmacol, 2014 May;66(5):646-57.
    PMID: 24329400 DOI: 10.1111/jphp.12192
    Objective: Examine the formation of pectin-insulin nanoparticles and their blood glucose lowering properties.

    Methods: The calcium pectinate nanoparticles were prepared by ionotropic gelation method, with alginate, sodium chloride or Tween 80 as additive. Their in vitro physicochemical, drug release and in vivo blood glucose lowering characteristics were evaluated.

    Key findings: Spherical calcium pectinate-insulin nanoparticles were characterized by size, zeta potential, insulin content and insulin association efficiency of 348.4 ± 12.9 nm, -17.9 ± 0.8 mV, 8.4 ± 1.0% and 63.8 ± 7.4%, respectively. They released less than 25% insulin following 24 h in simulated intestinal medium and exhibited delayed blood glucose lowering effect in rats. Incorporation of solubilizer sodium chloride or Tween 80 into nanoparticles did not enhance blood glucose lowering capacity owing to sodium chloride reduced matrix insulin content and Tween 80 interacted with water and had its blood glucose dilution effect negated. Combination of nanoparticles with alginate gel to allow prolonged intestinal residence and more insulin release did not enhance their blood glucose lowering capacity because of calcium alginate-cross-linked gel formation that could retard insulin release and migration into systemic circulation.

    Conclusion: Physicochemical responses of additives in vivo affected blood glucose regulation property of pectin-insulin nanoparticles.

    Keywords: Tween 80; alginate; insulin; nanoparticle; pectin.
    Matched MeSH terms: Diabetes Mellitus/drug therapy
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links