Herbal treatment for diabetes mellitus is widely used. The pharmacological activity is thought to be due to the phenolic compounds found in the plant leaves. The present study aims to investigate the ...phytochemical composition of
(UD) hydroethanolic extract and to screen its antidiabetic activity by disaccharidase hindering and glucose transport in Caco-2 cells. The results have shown that a total of 13 phenolic compounds in this work, viz. caffeic and coumaric acid esters (
,
,
-
,
), ferulic derivative (
), and flavonoid glycosides (
,
,
-
), were identified using HPLC-DAD-ESI/MS
. The most abundant phenolic compounds were
(rutin) followed by
(caffeoylquinic acid III). Less predominant compounds were
(caffeoylquinic acid II) and
(kaempferol-O-rutinoside). The UD hydroethanolic extract showed 56%, 45%, and 28% (1.0 mg/mL) inhibition level for maltase, sucrase, and lactase, respectively. On the other hand, glucose transport was 1.48 times less at 1.0 mg/mL UD extract compared with the control containing no UD extract. The results confirmed that
is a potential antidiabetic herb having both anti-disaccharidase and glucose transport inhibitory properties, which explained the use of UD in traditional medicine.
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Nanotechnology is a continually growing field with a wide range of applications from food science to biotechnology and nanobiotechnology. As the current world is grappling with ...non-biodegradable waste, considered more challenging and expensive to dispose of than biodegradable waste, new technologies are needed today more than ever. Modern technologies, especially nanotechnology, can transform biodegradable waste into products for human use. Researchers are exploring sustainable pathways for nanotechnology by utilizing biodegradable waste as a source for preparing nanomaterials. Over the past ten years, the biogenic production of metallic nanoparticles (NPs) has become a promising alternative technique to traditional NPs synthesis due to its simplicity, eco-friendliness, and biocompatibility in nature. Fruit and vegetable waste (after industrial processing) contain various bioactives (such as flavonoids, phenols, tannins, steroids, triterpenoids, glycosides, anthocyanins, carotenoids, ellagitannins, vitamin C, and essential oils) serving as reducing and capping agents for NP synthesis and they possess antibacterial, antioxidant, and anti-inflammatory properties. This review addresses various sources of biogenic NPs including their synthesis using fruit/vegetable waste, types of biogenic NPs, extraction processes and extracted biomaterials, the pharmacological functionality of NPs, industrial aspects, and future perspectives. In this manner, this review will cover the most recent research on the biogenic synthesis of NPs from fruit/vegetable peels to transform them into therapeutic nanomedicines.
Oxidative stress (OS) is a cytopathic outcome of excessively generated reactive oxygen species (ROS), down regulated antioxidant defense signaling pathways, and the imbalance between the produced ...radicals and their clearance. It plays a role in the genesis of several illnesses, especially hyperglycemia and its effects. Diabetic retinal illness, a micro vascular side effect of the condition, is the prime reason of diabetic related blindness. The OS (directly or indirectly) is associated with diabetic retinopathy (DR) and related consequences. The OS is responsible to induce and interfere the metabolic signaling pathways to enhance influx of the polyol cascades and hexosamine pathways, stimulate Protein Kinase-C (PKC) variants, and accumulate advanced glycation end products (AGEs). Additionally, the inequity between the scavenging and generation of ROS is caused by the epigenetic alteration caused by hyperglycemia that suppresses the antioxidant defense system. Induced by an excessive buildup of ROS, retinal changes in structure and function include mitochondrial damage, cellular death, inflammation, and lipid peroxidation. Therefore, it is crucial to comprehend and clarify the mechanisms connected to oxidative stress that underlie the development of DR.
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•Conceptual understanding of oxidative stress.•Pathological understanding of diabetic retinopathy.•A correlative understanding of stress and retinopathy at molecular level.•A detailed description on reactive oxygen species, retinal changes and abnormal functionality of mitochondria.
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Various neurodegenerative diseases (parkinson, huntington, alzheimer, and amyotrophic lateral sclerosis) are becoming serious global health challenges. Despite various treatment ...options, successful delivery and effective outcomes have been challenged with several physiological-anatomical barriers, formulation related issues, post-administration hurdles, regulatory constraints, physical hurdles, environmental issues, and safety concern. In the present review, we addressed a brief understanding of pathological and normal condition of blood brain barrier (BBB), rational for brain delivery using nanocarriers, major challenges, advantages of nanomedicine, critical aspects of nanomedicine to translate from bed to clinics, and strategic approaches for improved delivery across BBB. The review addressed various mechanistic perspective for delivery of drug loaded nanocarriers across BBB. Moreover, several reports have been published wherein phytomedicine, exosomes, magnetic nanopartilces, functionalized nanocarriers, cationic nanopartilces, and nano-phytomedicine were investigated for remarkable improvement in neurological disorders. These findings are informative for healthcare professionals, researchers, and scientists working in the domains. The successful application and convincing outcomes of nanomedicines were envisaged with clinical trials conducted on various drugs intended to control neurological disorders (NDs). Conclusively, the review addressed comprehensive findings on various aspects of drug loaded nanocarrier delivery across BBB, considerable risks, potential therapeutic benefits, clinical trial based outcomes, and recent advances followed by future perspectives.
Inflammation is responsible for the development of many diseases that make up a significant cause of death. The purpose of the study was to develop a novel nanophytosomal preparation of ...epigallocatechin-3-gallate (EGCG) and egg phospholipid complex that has a lower particle size with higher drug loading capability, physical stability and anti-inflammatory activities. The impact of different factors and material characteristics on the average particle size was studied along with the drug loading of phytosome using design of experiment (DoE). The in vivo anti-inflammatory study was evaluated using a rat model to investigate the performance of EGCG nanophytosome. UHPLC results showed that 500 µg of EGCG were present in 1 mL of green tea extract. SEM data exhibited that phytosome (phospholipid-drug complex) was in the nanosize range, which was further evident from TEM data. Malvern Zetasizer data showed that the average particle size of the EGCG nanophytosome was in the range of 100-250 nm. High drug loading (up to 90%) was achieved with optimum addition rate, stirring temperature and phospholipid concentration. Stability study data suggest that no significant changes were observed in average particle size and drug loading of nanophytome. The in vivo anti-inflammatory study indicated a significant anti-inflammatory activity of green tea extract, pure EGCG and its phytosomal preparations (
≤ 0.001) against acute paw edema.
Acyclovir (ACV) controls cutaneous herpes, genital herpes, herpes keratitis, varicella zoster, and chickenpox. From previously reported ACV formulations, we continued to explore the permeation ...behavior of the optimized ACV loaded optimized ethosome (ETHO2R) and elastic liposome (ELP3R) and their respective carbopol gels across artificial membrane, cultured human EpiDerm, and rat skin. Transepidermal water loss (TEWL), scanning electron microscopy (SEM), confocal laser scanning microscopy (CLSM), and atomic force microscopy (AFM) were used to investigate the mechanistic perspective of permeation behavior. The size values of reformulated ELP3-R and ETHO2-R were observed as 217 and 128 nm, respectively (close to previous report), whereas their respective gels showed as 231 and 252 nm, respectively. ETHO2R showed high elasticity, %EE, and low vesicle size. These were investigated for the diffusion rate of the drug permeation (3 h) across the artificial membrane, cultured human EpiDerm, and rat skin. ETHO2GR showed the highest permeation flux (78.42 µg/cm2/h), diffusion coefficient (8.24 × 10−5 cm2/h), and permeation coefficient (0.67 × 10−3 cm/h) of ACV across synthetic membrane, whereas diffusion coefficient (2.4 × 10−4 cm2/h) and permeation coefficient (0.8 × 10−3 cm/h) were maximum across EpiDerm for ETHO2GR. ETHO2R suspension showed maximized permeation flux (169.58 µg/cm2/h) and diffusion rate (0.293 mg/cm2/h1/2), suggesting the rapid internalization of vesicles with cultured skin cells at low viscosity. A similar observation was revealed using rat skin, wherein the permeation flux (182.42 µg/cm2/h), permeation coefficient (0.3 × 10−2 cm/h), and diffusion rate (0.315 mg/cm2/h1/2) of ETHO2R were relatively higher than ELP3R and ELP3GR. Relative small size (128 nm), low viscosity, ethanol-mediated ultra-deformability, high drug entrapment (98%), and elasticity (63.2) are associated with ETHO2R to provide remarkable permeation behavior across the three barriers. The value of TEWL for ETHO2R (21.9 g/m2h) was 3.71 times higher than untreated control (5.9 g/m2h), indicating ethanol-mediated maximized surficial skin lipid perturbation at 3 h of application, whereas the respective ETHO2GR-treated rat skin had TEWL value (18.6 g/m2h) slightly lower than ETHO2R due to gel-based hydration into the skin. SEL, CLSM, and AFM provided a mechanistic perspective of ETHO2R and ELP3R-mediated permeation across rat skin and carrier-mediated visualization (skin–vesicle interaction). AFM provided detailed nanoscale surface roughness topographical parameters of treated and untreated rat skin as supportive data to SEM and CLSM. Thus, ethosomes ETHO2R and respective gel assisted maximum permeation of ACV across rat skin and cultured human EpiDerm to control cutaneous herpes infection and herpes keratitis.
This study investigated enhanced bioavailability and sustained delivery of transdermally delivered rifampicin (RIF) in elastic liposomes (ELs). F3, F5, and F7 were optimized formulations comprising ...of 200, 140 and 80 mg of tween 80, respectively, and PhospholiponⓇ 90 G (300 mg). They were optimized based on in vitro and ex vivo parameters. Using the Franz diffusion cell, an ex vivo study was conducted by utilizing the rat skin for permeation profiles. Also, pharmacokinetic parameters, mechanistic evaluation of penetration, and histopathological investigation were conducted in the rat model for complete dynamic evaluations. Vesicle sizes of suspensions and gels were found to be similar whereas zeta potential of gel attained more negativity due to acidic carbopol. Permeation parameters of gels were significantly (p < 0.05) higher compared to respective ELs due to increased residence time and the composition of the formulations (ethanol, tween 80, d-limonene and lipid). Bioavailability of RIF (F5 gel) was improved by transdermal absorption as evidenced with AUC0→24 of transdermal F5 gel (56.23±2.7 µg.hr/mL) and oral drug suspension (41.71±5.2 µg.hr/mL). A lower value of transdermal Cmax (6.9 ± 0.8 µg/mL) validated sustained delivery for improved tuberculosis management than oral delivery (10.5 ± 1.46.9 ± 0.8 µg/mL). In vivo skin interaction, biopsy and in silico prediction studies corroborated suitable alternative for sustained and prolonged delivery of RIF with high patient compliance to control cutaneous tuberculosis and related infections.
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In the last few decades, solid dispersion (SD) technology had been studied as an approach to produce an amorphous carrier to enhance the solubility, dissolution rate, and bioavailability of poorly ...water-soluble drugs. The use of suitable carrier and methodology in the preparation of SDs play a significant role in the biological behavior of the SDs. SDs have been prepared using a variety of pharmaceutically acceptable polymers utilizing various novel technologies. In the recent years, much attention has been paid toward the use of novel carriers and methodologies in exploring novel types of SDs to enhance therapeutic efficacy and bioavailability. The use of novel carriers and methodologies would be very beneficial for formulation scientists to develop some SDs-based formulations for their commercial use and clinical applications. In the present review, current literature of novel methodologies for SD preparation to enhance the dissolution rate, solubility, therapeutic efficacy, and bioavailability of poorly water-soluble drugs has been summarized and analyzed. Further, the current status of SDs, patent status, and future prospects have also been discussed.
The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used ...for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.
The purpose of the present study was to improve the aqueous solubility, dissolution, and antioxidant activity of the water-insoluble drug piperine (PIP). The study was performed by preparing PIP ...binary inclusion complex (PIP BIC) and piperine ternary inclusion complex (PIP TIC) by different methods. The effect of a hydrophilic auxiliary substance (TPGS) was assessed with addition to PIP and hydroxypropyl beta cyclodextrin (HP β CD) complex. The phase solubility study was performed to evaluate the complexation efficiency and stability constant. The aqueous solubility, dissolution, physicochemical assessment, antioxidant activity, antimicrobial activity, and molecular docking were further evaluated to check the effect of the complexation of PIP. The stability constant (Ks) value was found to be 238 and 461 M
for the binary and ternary inclusion complex. The dissolution study results showed a marked enhancement of release in comparison to pure drug. XRD and SEM studies revealed the presence of more agglomerated and amorphous structures of PIP, which confirmed the formation of complexes. The results of DPPH radical scavenging and antimicrobial activity showed a significant (
< 0.05) enhancement in scavenging activity for PIP TIC (microwave irradiation (MI)). The docking studies have revealed that the binding affinity of TPGS at the PIP-HP β CD complex was -5.2 kcal/mol.
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