Search

Pullulan, a natural polysaccharide with unique biocompatibility and biodegradability, has gained prominence in nanomedicine. Its application in nanoparticle drug delivery systems showcases its potential for precision medicine. Aim of Study: This scientific review aims to comprehensively discuss and summarize recent advancements in pullulan-based polymeric nanoparticles, focusing on their formulation, characterization, evaluation, and efficacy. Methodology: A search on Scopus, PubMed, and Google Scholar, using "Pullulan and Nanoparticle" as keywords, identified relevant articles in recent years. Results: The literature search highlighted a diverse range of studies on the pullulan-based polymeric nanoparticles, including the success of high-selectivity hybrid pullulan-based nanoparticles for efficient boron delivery in colon cancer as the active targeting nanoparticle, the specific and high-efficiency release profile of the development of hyalgan-coated pullulan-based nanoparticles, and the design of multifunctional microneedle patches that incorporated pullulan–collagen-based nanoparticle-loaded antimicrobials to accelerate wound healing. These studies collectively underscore the versatility and transformative potential of pullulan-based polymeric nanoparticles in addressing biomedical challenges. Conclusion: Pullulan-based polymeric nanoparticles are promising candidates for innovative drug delivery systems, with the potential to overcome the limitations associated with traditional delivery methods. [ABSTRACT FROM AUTHOR]

Antioxidants are essential for reducing oxidative stress, protecting cells from damage, and supporting overall well-being. Functionalized mesoporous silica materials have garnered interest due to their flexible uses in diverse domains, such as drug delivery systems. This review aims to thoroughly examine and evaluate the progress made in utilizing functionalized mesoporous silica materials as a possible approach to enhancing antioxidant activity. The authors performed a thorough search of reliable databases, including Scopus, PubMed, Google Scholar, and Clarivate Web of Science, using precise keywords linked to functionalized mesoporous silica nanoparticles and antioxidants. The identified journals serve as the major framework for the main discussion in this study. Functionalized mesoporous silica nanoparticles have been reported to greatly enhance antioxidant activity by allowing for an increased loading capacity, controlled release behavior, the targeting of specific drugs, improved biocompatibility and safety, and enhanced penetration. The results emphasize the significant capacity of functionalized mesoporous silica (FSM) to bring about profound changes in a wide range of applications. FSM materials can be designed as versatile nanocarriers, integrating intrinsic antioxidant capabilities and augmenting the efficacy of current drugs, offering substantial progress in antioxidant therapies and drug delivery systems, as well as enhanced substance properties in the pharmaceutical field. Functionalized mesoporous silica materials are a highly effective method for enhancing antioxidant activity. They provide new opportunities for the advancement of cutting-edge treatments and materials in the field of antioxidant research. The significant potential of FSM materials to change drug delivery methods and improve substance properties highlights their crucial role in future breakthroughs in the pharmaceutical field and antioxidant applications. [ABSTRACT FROM AUTHOR]

Phytochemicals have shown potentials in preventing and treating various lung diseases, including asthma and lung cancer. However, their use has been hampered by limitations such as poor water solubility and instability. Nanoformulations, which include organic nanoparticles (e.g. liposomes) and inorganic nanoparticles (e.g. gold/silver nanoparticles) have potential to enhance drug solubility and subsequently increase their absorption and bioavailability. These drug formulations can be administered via various routes such as oral, intravenous, and pulmonary. This review highlights the potential of some phytochemicals in managing lung diseases and discusses the mechanism of actions of these phytochemicals and the impact of using the nanoformulations to deliver phytochemicals, particularly through pulmonary route. While pre-clinical studies have shown promising therapeutic activities of phytochemicals-loaded nanoformulations, further research is required. In conclusion, the application of phytochemicals and nanoformulations as drug delivery systems could be a promising approach to facilitate optimal therapy for lung diseases. [ABSTRACT FROM AUTHOR]

Purpose: Cisplatin (CDDP), while amongst the recognised chemotherapeutic drugs currently available, is known to have limitations; the lack of a single treatment approach and non-specific targeted therapies. Therefore, the development of an innovative strategy that could achieve localised CDDP treatment is an urgent undertaking. Recent advances in titania nanotube arrays (TNAs) technology have demonstrated promising applications for localised chemotherapeutic drug treatment. The present work investigated the efficiency of a TNA nanosystem for the localised CDDP treatment of nasopharyngeal carcinoma (NPC). Methods: Two models of the TNA nanosystem were prepared: CDDP loaded onto the TNA nanosystem surface (CDDP-TNA) and the other consisted of chitosan-coated CDDP-TNA. CDDP release from these two nanosystems was comprehensively tested on the NPC cells NPC/HK-1 and C666-1. The NPC cytotoxicity profile of the two CDDP-TNA nanosystems was evaluated after incubation for 24, 48 and 72 hours. Intracellular damage profiles were studied using fluorescence microscopy analysis with Hoechst 33342, acridine orange and propidium iodide. Results: The half-maximal inhibitory concentrations (IC50) of CDDP at 24 hours were 0.50 mM for NPC/HK-1 and 0.05 mM for C666-1. CDDP in the CDDP-TNA and chitosan-coated CDDPTNA models presented a significant degree of NPC inhibition (P < 0.05) after 24, 48 and 72 hours of exposure. The outcome revealed cellular damage and shrinkage of the cell membranes after 48 hours of exposure to CDDP-TNA. Conclusion: This in vitro work demonstrated the effectiveness of TNA nanosystems for the localised CDDP treatment of NPC cells. Further in vivo studies are needed to support the findings. [ABSTRACT FROM AUTHOR]

Drug stability is one of the most important criteria for producing safe, excellent, and effective products. Some environmental factors that influence drug stability are light, temperature, and humidity. Simvastatin is a cholesterol-lowering drug that is known to be sensitive to high temperatures and humidity. The purpose of this study is to analyze the effect of 6 months of real-time storage conditions on the stability of generic simvastatin tablets in public pharmacy facilities. This study used a simulation method with 4 brands of simvastatin generic tablets with two different strengths (10 mg and 20 mg). In the process, the sample was conditioned in 6 different regions for 6 months. The results of temperature and humidity monitoring showed 2 locations at ≤ 25°C, 4 locations had a temperature of ≥ 25°C and all locations had humidity > 65 %. The drug was evaluated for physical and chemical quality parameters at months 0, 3, and 6. After being stored for 6 months, the tablets showed a decrease in disintegration time and an increase in friability, showing a lack of durability. Similarly, there was a decrease in the content concentration in the tablets but fortunately, the level was still within the accepted specification range (90 - 110 %). However, there was one tablet that did not meet the dissolution test requirements after the storage duration (Q ≤ 75 % at 30 min). The results of the stress test showed that simvastatin degraded in all conditions. This stress test confirmed the extreme instability of simvastatin. Poor storage conditions can reduce the quality of generic simvastatin tablets, thus a well-controlled environment is vital in pharmacy facilities. [ABSTRACT FROM AUTHOR]

Chitosan has been shown to have great potentials in various pharmaceuticals and biomedical applications, including drug delivery. Derived from chitin abundantly available in the shells of crustaceans such as crabs and shrimps, this naturally occurring polysaccharide is classified based on its molecular weight: low, medium or high. This study aimed to explore the production of chitosan nanoparticles (NP) and the influence of different factors on the physical properties of the NP produced. These factors were the concentrations of acetic acid, chitosan flakes and tripolyphosphate (TPP). The design of experiment (DoE) approach was used to determine the optimum conditions for the production of chitosan NP, with particle size (nm) and polydispersity index (PdI) being set as the responses. The chitosan flakes were solubilised in acetic acid at a specific concentration determined by the DoE before dropwise addition of TPP in an ice bath. The mixture was stirred at room temperature and subsequently centrifuged to remove the unformed materials, and then was spray-dried into powder. The size, surface charge, shape and morphology of the particles produced were characterised and infrared analysis was conducted. The results showed that the particles were spherical, slightly positively charged (ζ-potential: +2.89 at pH 7) and the infrared analysis displayed important peaks of the chitosan NP. The DoE results showed that not all combinations of parameters could produce NP; hence, determination of concentration for each parameter is essential. The equation produced by the DoE will be a useful guide to minimise error in this circumstance. In conclusion, the acetic acid and chitosan flakes concentrations were found to influence the particle size positively, whilst the increment in TPP concentration will adversely affect the particle size. Similar pattern of response was also observed for the PdI of the particles. The methods used in this study has successfully produced spherical particles, with evidence of interactions between TPP and chitosan in the NP as shown in the infrared spectrum. [ABSTRACT FROM AUTHOR]

Despite the conventional treatment combining chemotherapy to a cytoreductive surgery, 60% of women suffered from ovarian cancer will relapse at the end of the treatment. Indeed, our main objective is to develop a targeted PDT treatment of peritoneal carcinomatosis from ovarian cancer to improve the life expectancy of cancer patients. For this, folic acid (FA) was used as a targeting agent, which can be coupled to photosensitizers (PS) to improve the selectivity towards cancer cells that over-expressed FR-α receptors, such as ovarian cancer cells. However, FA can undergo some stability issues. We conducted a Design of Experiment (DoE to understand the parameters influencing the degradation of FA. Factors such as light, oxygen, time of storage, temperature and type of medium were evaluated FA-PS conjugates were also tested to determine the influence of PS type on the stability of FA. FA-PS conjugates demonstrated different photostability, in comparison to FA.. FA-PEG-pyropheophorbide a demonstrates the best photostability. According to the DOE), after more than 80 experimental screenings, temperature, storage time and type of medium were found to be the most influencial parameters on the degradation of FA. FA moleculesalso demonstrated weaker photostability as compared to FA-PEG-pyropheophorbide a , which is an advantage for the efficiency of PDT. [ABSTRACT FROM AUTHOR]

Rifampicin and isoniazid are two of the first-line drugs used to treat tuberculosis (TB). Rifampicin is sensitive to light, heat and moisture, and is also known to have poor solubility which affects the absorption of the drug in the gastrointestinal tract. This study was conducted to investigate the effects of different types of Eudragit® in the formulation of microparticles of rifampicin and isoniazid. Two types of Eudragit were used which are Eudragit RL-PO and Eudragit RS-PO. The particle size of rifampicin microparticles for Eudragit RL-PO and Eudragit RS-PO were recorded at 44 µm and 64 µm, respectively. Isoniazid microparticles were found to have volume mean diameters of 63 µm and 54 µm for formulations incorporated with Eudragit RL-PO and Eudragit RS-PO, respectively. Eudragit RL-PO formulated rifampicin microparticles encapsulated 80.8% and 23.3% for those formulated with Eudragit RS-PO. Isoniazid microparticles recorded an encapsulation efficiency of 98.7% and 61.9% in formulations using Eudragit RL-PO and Eudragit RS-PO correspondingly. The formulations retained some of the functional groups, but changes were also observed. Scanning electron microscope (SEM) shows consistently spherical and porous microparticles with rough surfaces. Dissolution studies indicate that isoniazid was released by Quasi-Fickian mechanism while rifampicin was released by non-Fickian mechanism. [ABSTRACT FROM AUTHOR]

Introduction: The classification of atovaquone (ATQ) as a BCS Class II drug illustrates its solubility challenges in the GIT that will affect its oral absorption and bioavailability. Among the polymers available for nanoparticles production, chitosan has demonstrated favorable properties, including biocompatibility and low toxicity. The objective of this study is to prepare and characterize chitosan nanoparticles as a carrier for ATQ with a specific aim for solubility enhancement. Methods: ATQ-loaded chitosan nanoparticles were prepared using the ionic gelation method. The formulations were characterized for particle size, polydispersity index (PDI), surface charge, encapsulation efficiency, FTIR spectroscopy, and in vitro drug release study in simulated gastric fluid (SGF; pH 1.2) and simulated intestinal fluid (SIF; pH 6.8). The stability of the nanoparticles was evaluated at 4°C, 25°C, and 40°C/75%RH for three months. Results: The physical properties of chitosan nanoparticles can be controlled by manipulating the components used in the formulation. The final formulation features: a particle size of 235.9 nm (± 4.9), PDI of 0.26 (± 0.02), zeta potential of +29.2 mV (± 1.1), and an encapsulation efficiency of 95.0% (± 1.0). In vitro drug release study showed a 7-fold and 4-fold increase in the solubility of ATQ in SGF and SIF respectively, as compared to the free drug. The aqueous nanoparticle formulations were stable for three months at 4°C and 25°C storage conditions. Conclusion: This study highlights the ability of chitosan nanoparticles to enhance the solubility of ATQ and potentially increase the bioavailability of ATQ in vivo. [ABSTRACT FROM AUTHOR]

Photodynamic therapy (PDT) is a cancer treatment modality that requires three components, namely light, dioxygen and a photosensitizing agent. After light excitation, the photosensitizer (PS) in its excited state transfers its energy to oxygen, which leads to photooxidation reactions. In order to improve the selectivity of the treatment, research has focused on the design of PS covalently attached to a tumor-targeting moiety. In this paper, we describe the synthesis and the physico-chemical and photophysical properties of six new peptide-conjugated photosensitizers designed for targeting the neuropilin-1 (NRP-1) receptor. We chose a TPC (5-(4-carboxyphenyl)-10,15, 20-triphenyl chlorine as photosensitizer, coupled via three different spacers (aminohexanoic acid, 1-amino-3,6-dioxaoctanoic acid, and 1-amino-9-aza-3,6,12,15-tetraoxa-10-on-heptadecanoic acid) to two different peptides (DKPPR and TKPRR). The affinity towards the NRP-1 receptor of the conjugated chlorins was evaluated along with in vitro and in vivo stability levels. The tissue concentration of the TPC-conjugates in animal model shows good distribution, especially for the DKPPR conjugates. The novel peptide-PS conjugates proposed in this study were proven to have potential to be further developed as future NRP-1 targeting photodynamic therapy agent. [ABSTRACT FROM AUTHOR]

Introduction: The glycolytic enzyme glyceraldehyde-3-phosphate dehydrogenase (GAPDH) can increase transferrin binding to M. tuberculosis cells and subsequently enhance iron absorption following GAPDH overexpression. The purpose of this paper is to study the binding interaction of the novel drug delivery of folic acid-isoniazid conjugates, which are α-folic acid conjugates ((4R)-4-[(4-{[(2-amino-4-oxo-3A-dihydropteridin-6 yl) methyI]amino}phenyI)formamido]-4-{[3 (4-{[(pyridin-4-yI)formohydrazIdo]carbonyI}-1H-1 carbamoyl}butanoic acid) and γ-folic acid conjugates (2-[(4-{[(2-amino-4-oxo-3A-dihydropteridin-7-yI)methyI]amino}phenyI)formamido]-4-{[3 (4-{[(pyridin-4-yI)formohydrazIdo]carbonyI}-1H-1 carbamoyl}butanoic acid). The conjugates are further investigated its ADMET profiles and its predicted pharmacokinetic to screen the overview of the behaviour of the drug in the body and to assess the effects or risks of these compounds on human body. Methods: The docking simulation files was prepared on AutoDock Tools 1.5.7 and the docking simulation was conducted using AutoDock 4 while the ADMET prediction was conducted using 3 different databases which are PreADME, SwissADME and ADMET Predictor X.4 ®. Results: The most important amino acid residue that formed hydrogen bond with both α-conjugate and γ-conjugate are ASN8, ARG78, and ASN33. The lowest binding affinity towards GAPDH are -6.20 kJ/mole and -6.37 kJ/mole for α-conjugate and γ-conjugate respectively. Both conjugates have ADMET risk score of 9 out of 22 which indicates the compounds are less likely to encounter ADMET problem. It also has low mutation risk of less than 1.0 of 5.4 which has the potential for microsomal activation for S.typhimurium strain and low toxicity risk of 1.5 out of 6.0 with the potential of inhibiting hERG and carcinogenicity in rat and positive Ames test (Salmonella typhimurium reverse mutation assay). Conclusion: The present study showed that both α-conjugate and γ-conjugate are favourable to bind to GAPDH and have low ADMET risk and mutation risk but are poorly absorbed by gastrointestinal. [ABSTRACT FROM AUTHOR]

Introduction: The therapeutic delivery nanosystem attracts major interest due to its potential in improving the effectiveness and minimising the drawback of treatments especially in the neuroscience field. This work investigates the potential of the titania nanotube arrays (TNA) nanosystem as the therapeutic delivery for resveratrol (RSV) to the neuronal cell line model. Methods: TNA was fabricated using electrochemical anodisation in an organic electrolyte, and the morphology of the nanotube structure was analysed using field-emission scanning electron microscopy. The dose-dependent study of SH-SY5Y cell lines was conducted by testing different concentrations of RSV for 24 h by using the tetrazolium inner salt (MTS reagent). The RSV release profile of the chitosan-coated TNA nanosystem was characterised in the biphasic condition of the sample immersed in phosphate-buffered saline at 37 °C. Subsequently, the functional analysis of RSV release from the TNA nanosystem by using an in-vitro cell culture model was characterised on the neuronal cell line model SH-SY5Y for 48 and 72 h. Results: Within the first 6 h and after 14 d, 23.41% ± 13.12% and approximately 49.01% ± 9.74%, respectively, of RSV were released from the chitosan-coated TNA nanosystem. SH-SY5Y cells were inhibited when cells were incubated in uncoated and chitosan-coated RSV-loaded TNA, thereby displaying the potential of TNA to load and release RSV in the in-vitro culture system. Conclusion: The findings from this study highlight the potential of TNA nanosystems to overcome the limitation in the delivery of the therapeutic compound especially in the neuroscience field. [ABSTRACT FROM AUTHOR]

Introduction: α-Mangostin (Amg), a compound isolated from the rind of the mangosteen (Garcinia mangostana L.), exhibits promising anticancer properties. However, its efficacy has been constrained by low solubility and selectivity towards cancer cells. To address this limitation, researchers have developed chitosan/alginate polymeric nanoparticles (NANO-AMCAL) to increase the efficiency of Amg. Initial in vitro research demonstrated the remarkable efficacy of NANO-AMCAL against breast cancer cells. The present study aims to assess NANO-AMCAL's potential for breast cancer treatment in Wistar rats (Rattus norvegicus) and determine the optimal dosage. Methods: Seven treatment groups, comprising normal (without DMBA induction), control, tamoxifen, Amg Pure (P.Amg), NANO-AMCAL 5 mg, NANO-AMCAL 10 mg, and NANO-AMCAL 20 mg, were established. The rats were subjected to subcutaneous administration of 7,12-dimethylbenz(a)anthracene (DMBA), a carcinogenic substance. Their body weight and tumor volume were measured every three days throughout the treatment period. On day 14, surgical procedures were conducted. Histopathological examinations were carried out on breast and lung tissues to assess the treatment's effectiveness. Results: The results showed that NANO-AMCAL significantly enhanced the anticancer activity of Amg in treating breast cancer in Wistar rats. NANO-AMCAL containing 0.33 mg of Amg had a healing effect three times better than 20 mg pure Amg and was comparable to tamoxifen. The effective dose of NANO-AMCAL for anti-breast cancer treatment in Wistar rats was found to be 20 mg, which exhibited a good healing response, and the tumor volume continued to decrease up to 17.43% on the 14th day. Furthermore, histopathological tests showed tissue repair and no metastases. Conclusion: These results imply that NANO-AMCAL could be a promising therapeutic choice for the treatment of breast cancer. [ABSTRACT FROM AUTHOR]