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Classification of infectious diseases based on their causative agents. The common infectious diseases include TB, pneumonia, HIV/AIDS, malaria, influenza, hepatitis, candidiasis and lymphatic filiariasis
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Most of the infectious diseases depending upon the stage of infection need treatment at least for a month to several years e.g. tuberculosis, acquired immunodeficiency syndrome. Medication by oral administration is of choice in all treatments, but unfortunately use of large doses resulting from drug poor solubility and bioavailability leads to toxi...
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New dianionic ionic liquids (ILs) based on carboxylic anions and ammonium cations were prepared and characterized. They were used as excipients to increase the solubility of two model oral drugs of BCS class II, ibuprofen and piroxicam. With only 0.2 mol% (≈100 mM) of [N4 1 1 2OH]2[C4H4O4], the solubility increases over 40-fold and 2-fold for ibupr...
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Purpose
The use of ionic liquids (ILs) in drug delivery has focused attention on non-toxic IL counterions. Cationic lipids can be used to form ILs with weakly acidic drugs to enhance drug loading in lipid-based formulations (LBFs). However, cationic lipids are typically toxic. Here we explore the use of lipoaminoacids (LAAs) as cationic IL counteri...
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Citations
... Its main function is to block the activity of reverse transcriptase. However, one limitation of nevirapine is its poor water solubility, which may impact its effectiveness [96]. Researchers used high-pressure homogenization and surface modification techniques, which are top-down methods, to produce nevirapine nanosuspensions. ...
The treatment of HIV presents significant challenges due to the low solubility and bioavailability of antiretroviral drugs. These limitations impact the absorption of the drugs in the gastrointestinal tract, leading to reduced effectiveness. Patients often exhibit varying responses due to inconsistent levels of the drug in their bloodstream. Achieving desired plasma concentrations is challenging and often requires higher doses that increase the risk of side effects. Developing drugs with low solubility is a complex and costly process, slowing down overall drug development. Traditional formulation strategies have proven ineffective in addressing these issues, necessitating exploration of innovative techniques. Nanocrystallization has emerged as a transformative approach that enhances solubility and dissolution rates by reducing drug particles to the nanometer scale. This increased surface area improves drug solubility and bioavailability. Nanocrystallized drugs demonstrate a faster onset of action, higher drug load, and enhanced safety and efficiency, offering a potential solution to the challenges posed by the poor water solubility of many antiretroviral drugs. This article delves into nanocrystal formulations of HIV drugs and examines the effectiveness of commonly used stabilizers and surfactants in nanocrystal production. The aim is to determine whether the popularization of nanocrystallization could potentially overcome the prevalent issues of low solubility and bioavailability in existing antiretroviral therapies.
... The characteristics of drug particles in the nanosuspension can be tailored to adapt to changes in the digestive environment, including pH, polymer compositions, surface-active agents, ionic strength, enzymatic activities, and gastrointestinal motility during absorption [27]. Additionally, they can be surface-modified to selectively adsorb blood proteins, targeting specific sites like the brain or bone marrow [28]. To maintain stability, nanosuspensions require a third component known as a stabilizer, such as a surfactant and/or polymer. ...
Objective: This study focuses on improving the delivery of Piribedil, a poorly soluble drug, to the brain through the nasal route using a nanosuspension in a nasal in-situ gel. Methods: The nanosuspension was prepared using the sonoprecipitation method. Quality-by-Design (QbD) principles were used to optimize both the formulation and process parameters. The optimal process parameters were determined as sonication time (7.09 min), sonication amplitude (83.44%), and infusion rate (2.41 mL/min) with a desirability value of 0.970. Results: The nanosuspension exhibited an average particle size ranging from 46.7 nm to 50.1 nm, and polydispersity index values between 0.393 and 0.425. Zeta potential values ranged from -33.78 ± 1.86 mV to -35.06 ± 2.12 mV, indicating favorable stability. FTIR studies revealed molecular interactions between Piribedil and stabilizers. XRPD and DSC analyses showed the transition from a crystalline to an amorphous state in the nanosuspension. Dissolution studies demonstrated significantly accelerated dissolution for the Piribedil nanosuspension, attributed to its nanosize and improved wettability. Stability assessments confirmed the robustness of the nanosuspension. Conclusion: This innovative approach offers potential solutions for drug solubility challenges and blood-brain barrier penetration, holding promise for effective brain-targeted treatments.
... The choice of nanoparticle shape and size depends on factors such as the intended drug delivery mechanism, target site, desired release profile, and stability considerations. 56,57 Nanosuspensions offer several advantages, including improved drug solubility, 58 enhanced bioavailability, controlled release of drugs, 59 and active ingredients. ...
Parasitic infections are a major global health issue causing significant mortality and morbidity. Despite substantial advances in the diagnostics and treatment of these diseases, the currently available options fall far short of expectations. From diagnosis and treatment to prevention and control, nanotechnology-based techniques show promise as an alternative approach. Nanoparticles can be designed with specific properties to target parasites and deliver antiparasitic medications and vaccines. Nanoparticles such as liposomes, nanosuspensions, polymer-based nanoparticles, and solid lipid nanoparticles have been shown to overcome limitations such as limited bioavailability, poor cellular permeability, nonspecific distribution, and rapid drug elimination from the body. These nanoparticles also serve as nanobiosensors for the early detection and treatment of these diseases. This review aims to summarize the potential applications of nanoparticles in the prevention, diagnosis, and treatment of parasitic diseases such as leishmaniasis, malaria, and trypanosomiasis. It also discusses the advantages and disadvantages of these applications and their market values and highlights the need for further research in this field.
... It minimizes the use of other excipients in the formulation in very high concentration. 4 It requires a very minimum concentration of suitable surfactants or suspending agents to stabilize the in aqueous or non-aqueous media. 5 A conventional pharmaceutical suspension may be a coarse dispersion in which uniform particles are dispersed in any vehicle. ...
... Nanotechnology-based medicine delivery systems have significantly improved healthcare and made it feasible to fight illnesses at the molecular level [30]. Nanoparticles are elegant vehicles for drug-targeted delivery because of their great stability and carrier capacity ( Figure 2) [31,32]. ...
... The utilization of nanoparticles for delivering drugs presents various benefits such as extended stability resulting in longer shelf life, significant capacity to carry drug molecules, the possibility of encapsulating both hydrophilic and hydrophobic substances, and versatility in administration methods, including oral intake and inhalation [30]. ...
... as extended stability resulting in longer shelf life, significant capacity to carry drug molecules, the possibility of encapsulating both hydrophilic and hydrophobic substances, and versatility in administration methods, including oral intake and inhalation [30]. ...
Tuberculosis (TB) is a serious infectious disease caused by Mycobacterium tuberculosis (MTB) and a significant health concern worldwide. The main threat to the elimination of TB is the development of resistance by MTB to the currently used antibiotics and more extended treatment methods, which is a massive burden on the health care system. As a result, there is an urgent need to identify new, effective therapeutic strategies with fewer adverse effects. The traditional medicines found in South Asia and Africa have a reservoir of medicinal plants and plant-based compounds that are considered another reliable option for human beings to treat various diseases. Abundant research is available for the biotherapeutic potential of naturally occurring compounds in various diseases but has been lagging in the area of TB. Plant-based compounds, or phytoproducts, are being investigated as potential anti-mycobacterial agents by reducing bacterial burden or modulating the immune system, thereby minimizing adverse effects. The efficacy of these phytochemicals has been evaluated through drug delivery using nanoformulations. This review aims to emphasize the value of anti-TB compounds derived from plants and provide a summary of current research on phytochemicals with potential anti-mycobacterial activity against MTB. This article aims to inform readers about the numerous potential herbal treatment options available for combatting TB.
... 7,8 The needs for Latin America were considered again in 2012. 9 Nifurtimox has been examined as a treatment for pediatric neuroblastoma 10,11 and other pediatric tumors, 12 and has also been patented as a drug to treat cancer and inhibit angiogenesis. 13 Nifurtimox is marketed by Bayer in the form of tablets (Lampit), to be administered for 90 days (acute infection) to 120 days (chronic infection), at a level of three tablets every day. ...
Nifurtimox is a nitroheterocyclic drug employed for treatment of trypanosomiases (Chagas disease and West African sleeping sickness); its use for certain cancers has also been assessed. Despite having been in the market for over 50 years, knowledge of nifurtimox is still fragmentary and incomplete. Relevant aspects of the chemistry and biology of nifurtimox are reviewed to summarize the current knowledge of this drug. These comprise its chemical synthesis and the preparation of some analogues, as well as its chemical degradation. Selected physical data and physicochemical properties are also listed, along with different approaches toward the analytical characterization of the drug, including electrochemical (polarography, cyclic voltammetry), spectroscopic (ultraviolet-visible, nuclear magnetic resonance, electron spin resonance), and single crystal X-ray diffractometry. The array of polarographic, ultraviolet-visible spectroscopic, and chromatographic methods available for the analytical determination of nifurtimox (in bulk drug, pharmaceutical formulations, and biological samples), are also presented and discussed, along with chiral chromatographic and electrophoretic alternatives for the separation of the enantiomers of the drug. Aspects of the drug likeliness of nifurtimox, its classification in the Biopharmaceutical Classification System, and available pharmaceutical formulations are detailed, whereas pharmacological, chemical, and biological aspects of its metabolism and disposition are discussed.
... These pathogens enter host systems through direct contact, inhalation, or ingestion. Phenomenal invasive mechanisms of infective pathogens and the tissue functional impairment and associated symptomatic diseases are growing day by day (Ranjita, 2013). The need for controlling the spread of highly virulent and contagious agents is the current pressing need for health-care professionals, researchers, and regulatory bodies. ...
... Results showed that this HYNIC-conjugated peptide was easily labeled with technetium-99m in high radiochemical yield ( Fig. 3 and Fig. 4) and was stable in saline (≥ 95%) and human serum (approximately ˃60%) up to 24 h and 4 h, respectively (Table 1 and Fig. 5). [ 99m Tc]Tc-M-7 showed high hydrophilicity, log p (− 4.29 ± 0.04), and water solubility that could be appropriate for overcoming the recurring problems of sub-optimal pharmacokinetics and low bioavailability [14,23]. ...
Purpose:
In this study, we designed a new linear 6-Hydrazinonicotinamide (HYNIC)-conjugated peptide (HYNIC-KRWrNM) (M-6) and labeled with technetium-99m for gamma imaging of glioblastoma as a αvβ3-positive tumor. We evaluated tumor targeting ability of this radio-peptide and compared with previous 99mTc-labeled HYNIC-conjugated RGD analogue peptides.
Procedures:
One new linear peptide (HYNIC-KRWrNM) (M-6) was designed and labeled with technetium-99m in the presence of 2-[[1,3-dihydroxy-2-(hydroxymethyl) propan-2-yl] amino] acetic acid (Tricine)/Ethylenediamine-N,N'-diacetic acid (EDDA) as co-ligand system. Then, this 99mTc-labeled peptide ([99mTc]Tc-M-7) was evaluated for in vitro stability in saline and serum, specific binding assay, internalization, and binding affinity (Kd). In addition, we performed biodistribution study and planar imaging on nude mice bearing U87-MG xenograft as a αvβ3-positive tumor.
Results:
The radiochemical yield of [99mTc]Tc-M-7 was obtained ˃95%. This 99mTc-labeled peptide remained stable and intact in saline solution after 24 h incubation. In addition, metabolic stability of this 99mTc-labeled peptide was obtained ˃60% after 4 h incubation in serum. The Kd value for [99mTc]Tc-M-7 was obtained 5.2 ± 1.0 nM. Based on biodistribution results in nude mice bearing U87-MG xenograft, tumor/muscle activity ratio was 6.22 and decreased to 1.89 in blocking group at the same time point (4 h p.i.). The blocking experiment results also indicated that tumor uptake and kidney uptake were αvβ3-mediated. In comparison with previous HYNIC-conjugated RGD analogue peptides, kidneys had the highest uptake of this 99mTc-labeled peptide (52.29 ± 11.48 at 1.5 h p.i. and 27.04 ± 0.66%ID/g at 4 h p.i.). Finally, similar to previous 99mTc-labeled HYNIC-conjugated RGD analogue peptides, [99mTc]Tc-M-7 showed acceptable tumor uptake after 4 h post-injection (based on ROI technique, target-to-background activity ratio = 3.80).
Conclusions:
This small linear 99mTc-labeled peptide, with high affinity to αvβ3 integrin, desirable water solubility, and cost efficient, demonstrates a potent tumor targeting ability as well as previous HYNIC-conjugated RGD analogue peptides. Hence, [99mTc]Tc-M-7 can be of service to as a new candidate for early detection of αvβ3-positive tumors.
... Two different LNC were selected and were characterized to select the one with the most suitable characteristics for this study. Several LNC have a size around 100 nm which can be expected to improve the bioavailability and therapeutic performance [35,36]. For optimized LNC, the obtained PdI were low, indicating narrow particle size distribution [37]. ...
The objective of this study was to develop clarithromycin-loaded lipid nanocarriers and incorporate them into microcapsules for pH-specific localized release of clarithromycin in the Helicobacter pylori microenvironment in order to obtain a gastro-retentive and pH-sensitive formulation. A Plackett-Burman design was applied to identify the effect of 5 factors on 3 responses. Then, a central composite design was applied to estimate the most important factors leading to the best compromise between lower particle size, polydispersity index and particle size changes. The optimized clarithromycin-loaded nanocapsules were employed to generate microcapsules by different methodologies. Nanocarriers and microcapsules were characterized in vitro. Experimental design and conditions were optimized to obtain nanocapsules of around 100 nm by a modified phase inversion-based process. High particle size homogeneity and high stability were achieved. At 4°C both optimized lipid nanocapsules were stable during at least 365 days, confirming stability under those conditions. Clarithromycin incorporation in the nanocarrier was effective. Both types of microcoating were evaluated regarding their pH sensitivity. Spray drying microcapsules exhibited similar and uncontrolled release profiles at pH 2 and 7.4. Alternatively, when microcoatings were generated using an Encapsulator, release was insignificant at pH 2, while at pH 7.4 release was triggered, and appeared more appropriate to formulate microcapsules that release nanocarriers under pH neutral Helicobacter pylori microenvironment conditions, thereby permitting effective drug delivery in infected locations. The release of clarithromycin from lipid nanocarrier loaded microcapsules was pH-sensitive suggesting that this could be an effective strategy for clarithromycin delivery to the Helicobacter pylori microenvironment. Clarithromycin nanocapsules with and without microcoating showed a high anti-Helicobacter pylori activity in vitro.
... It is a class II drug, classified as a very poorly soluble drug [77,81]. It is a class III drug [82,83]. Has antitumor activity [84], but it is potentially effective in combating all evolutionary forms of T. cruzi [85]. ...
Introduction
Many drugs used to combat schistosomiasis, Chagas disease, and leishmaniasis (SCL) have clinical limitations such as: high toxicity to the liver, kidneys and spleen; reproductive, gastrointestinal, and heart disorders; teratogenicity. In this sense, drug delivery systems (DDSs) have been described in the literature as a viable option for overcoming the limitations of these drugs. An analysis of the level of development (TRL) of patents can help in determine the steps that must be taken for promising technologies to reach the market.
Areas covered
This study aimed to analyze the stage of development of DDSs for the treatment of SCL described in patents. In addition, we try to understand the main reasons why many DDSs do not reach the market. In this study, we examined DDSs for drugs indicated by WHO and treatment of SCL, by performing a search for patents.
Expert opinion
In this present work we provide arguments that support the hypothesis that there is a lack of integration between academia and industry to finance and continue research, especially the development of clinical studies. We cite the translational research consortia as the potential alternative for developing DDSs to combat NTDs.