Release Of Active Ingredients Research Articles

Alloy nanozyme-reinforced hyaluronic acid-based hydrogel with wound environment-responsive properties for synergistically accelerating infectious wound healing

The recovery of infectious wound tissues presents a significant global health challenge due to the impediments posed by the harsh healing microenvironment, which includes ongoing bacterial invasion, high oxidative stress, inflammatory response, and impaired angiogenesis. To overcome the above issues, we propose a composite hydrogel based on the multiple-crosslinked mechanism involving the covalent network of CC bonds within catechol and maleic-modified HA (CMHA), the self-assembly network of glycyrrhizic acid (GA), and the metal-polyphenol coordination induced by ZHMCe for accelerating infectious wound healing. The resulting CMHA/GA/ZHMCe hydrogels demonstrate enhanced mechanical, adhesive, antioxidative, and antibacterial properties. Importantly, the hydrogel system possesses wound environment-responsive properties that allow it to adapt to the specific therapeutic requirements of different stages by regulating various enzyme activities in the healing of infected wounds. Furthermore, the biocompatible CMHA/GA/ZHMCe shows the ability to promote cell migration and angiogenesis in vitro while reprogramming macrophages toward an anti-inflammatory phenotype due to the effective release of active ingredients. In vivo experiments confirm that the CMHA/GA/ZHMCe hydrogel significantly enhances infectious wound healing by accelerating re-epithelialization, promoting collagen deposition, regulating inflammation, and contributing to vascularization. These findings underscore the therapeutic potential of our hydrogel dressings for the treatment of bacterially infected cutaneous wound healing.

Plant-based delivery systems for controlled release of hydrophilic and hydrophobic active ingredients: Pea protein-alginate bigel beads

Oral delivery systems for nutrients and nutraceuticals are required for personalized nutrition applications. In some applications, these delivery systems need to encapsulate both hydrophilic and hydrophobic bioactive agents. In this study, bigel beads (2 mm) were prepared using pea protein (PP) and sodium alginate (SA) to form the hydrogel phase, and glyceryl monostearate and soybean oil to form the oleogel phase. The hydrogel phase was crosslinked by using Ca2+ ions to form electrostatic bridges between the alginate molecules. The bigel beads had an oil-in-water type structure consisting of an oleogel dispersed phase within a hydrogel continuous phase. These beads were used to encapsulate and control the release of model hydrophobic (curcumin) and hydrophilic (epigallocatechin gallate) nutraceuticals. The textural and microstructural characteristics of the bigel beads were evaluated by dynamic shear rheology, textural profile analysis, cryo-electron microscopy, and fluorescence confocal microscopy. As the concentration of SA increasing from 0.2 to 1.0%, the hardness of bigel beads increased from 306.75 g to 792.40 g. In vitro digestion experiments showed that most of the nutraceuticals were released in the small intestine, rather than the stomach. Nutraceutical release could be controlled by manipulating bead composition, with the extent of nutraceutical release decreasing with increasing alginate concentration. The bigel beads developed in this study could be used as easy-to-swallow carriers for the controlled release of hydrophilic and hydrophobic bioactive ingredients. These kinds of products may be especially useful for people with dysphagia.

A bio-degradable, triboelectric self-stimulated herbal transdermal therapeutic dressing for healing massive chronic wound

Homogeneous controlled release of active ingredients, avoiding secondary damage of dressing changes would be considerable advance for transcutaneous drug delivery treatment. Here, a bio-degradable, self-stimulated herbal transdermal therapeutic dressing (irritability) driven by multi-ball nimble-rolling triboelectric nanogenerator (mbnr-TENG) is proposed that provided a stable and adjustable triboelectric field for controlling drug release. The mbnr-TENG deliver a periodic triboelectric field of 140 V for herbal dressings by collecting human mechanical energy to enhance transdermal properties of total flavonoids and chlorogenic acid in ss-HTTD by 310% and 147%. Following a therapeutic cycle using ss-HTTD, the secretion of inflammatory factors decreased by 50.35%, and wound healing rate increased by 24.98%, then completely degraded after 10 days. As a new drug delivery system, this work holds great potential in healing massive chronic wound, ss-HTTD is advantageous in controlling drug release, enhancing the activity and the long-term stability of herbal medicines.

Fabrication of pH-responsive nanoparticles for co-delivery of fungicide and salicylic acid with synergistic antifungal activity

Stimuli-responsive co-delivery nanopesticides with different action mechanisms have received widespread attention due to the improved bioactivity, long effective duration, and reduced risks to the environment. Herein, fungicide tebuconazole (TEB) and plant immune inducer poly(salicylic acid) (PSA) co-assembled nanoparticles (TP NPs) are fabricated through non-covalent interactions without the use of any adjuvants. The results show that the obtained TP NPs have excellent physicochemical properties, displaying uniform morphology with an average particle size of 152 nm, low PDI (0.064), and high surface activity. The TP NPs exhibit acid-responsive behaviors, enabling the intelligent release of active ingredients in the specific acidic microenvironment caused by the invasion of plant pathogens. In vitro fungicidal activities of TP NPs are 1.9 and 1.6 times higher than TEB technical against Sclerotinia sclerotiorum and Fusarium graminearum respectively. Additionally, the stimuli-responsive co-delivery fungicidal nanosystem not only has a longer effective duration compared to both TEB technical and TP Mix but also significantly reduces the genetic toxicity of TEB to the plants. Therefore, this fungicide and plant immune inducer co-delivery nanosystem provides a novel strategy for development of multimode synergetic nanopesticide and sustainable plant disease management.

Photothermal controlled antibacterial Ta4C3Tx-AgNPs/nanocellulose bioplastic food packaging

Uncontrolled antibacterial, insufficient barrier and low strength are the bottlenecks of food packaging applications. Herein, Ta4C3Tx nanosheet as a template was used to prepare Ta4C3Tx immobilized silver nanoparticles (Ta4C3Tx-AgNPs), which was compounded with nanocellulose to obtain high-strength and high barrier controllable bactericidal nanocellulose-based bioplastic packaging (CTa-Ag). The results indicated that due to the hydrogen bonding between nanocellulose and Ta4C3Tx, the bridging effect of QCS (quaternized chitosan) and the filling of Ta4C3Tx-AgNPs, the CTa-Ag had tightly stacked microstructure, which endowed them with excellent mechanical properties (4.0 GPa), ultra-low oxygen permeability (0.009 cm3/m2·d·atm) and stable photothermal conversion efficiency. Importantly, the packaging exhibits the ability to control the release of antibacterial active ingredients. Moreover, the synergistic effects of controllable release of nano active factors, photothermal and photocatalysis in CTa-Ag gave it long-lasting antibacterial properties. This study brings new insights into the design and manufacture of multifunctional, controllable and long-lasting antibacterial bioplastic food packaging.

Unraveling the Therapeutic Prospects of Solid Lipid Nanoparticles for the Treatment of Parasitic Diseases

Parasites induce a spectrum of illnesses, ranging from mild to severe, often causing significant global outbreaks. Existing antiparasitic drugs exhibit toxicity and notable side effects. Nanocarriers offer a promising solution by mitigating these issues through reduced side effects, enhanced target delivery, and additionally regulated prolonged active ingredient release. Solid lipid nanoparticles (SLNs), a subset of lipid nanoparticles (LNPs), have gained prominence for their favorable attributes. SLNs present themselves as a feasible option among colloidal carriers, offering an optimal release rate, stability, and precise target delivery. Their potential to deliver natural antiparasitic products is particularly noteworthy. Recent advancements in utilizing nanoparticles to enhance SLN stability and loading capacity are also explored in this review. The narrative encompasses SLN development, preparation methods, characterization, and the incorporation of drugs for combating parasitic diseases, offering insights into the evolving landscape of antiprotozoal SLN-saturated medications

Co-Assembly of Cancer Drugs with Cyclo-HH Peptides: Insights from Simulations and Experiments.

Peptide-based nanomaterials can serve as promising drug delivery agents, facilitating the release of active pharmaceutical ingredients while reducing the risk of adverse reactions. We previously demonstrated that Cyclo-Histidine-Histidine (Cyclo-HH), co-assembled with cancer drug Epirubicin, zinc, and nitrate ions, can constitute an attractive drug delivery system, combining drug self-encapsulation, enhanced fluorescence, and the ability to transport the drug into cells. Here, we investigated both computationally and experimentally whether Cyclo-HH could co-assemble, in the presence of zinc and nitrate ions, with other cancer drugs with different physicochemical properties. Our studies indicated that Methotrexate, in addition to Epirubicin and its epimer Doxorubicin, and to a lesser extent Mitomycin-C and 5-Fluorouracil, have the capacity to co-assemble with Cyclo-HH, zinc, and nitrate ions, while a significantly lower propensity was observed for Cisplatin. Epirubicin, Doxorubicin, and Methorexate showed improved drug encapsulation and drug release properties, compared to Mitomycin-C and 5-Fluorouracil. We demonstrated the biocompatibility of the co-assembled systems, as well as their ability to intracellularly release the drugs, particularly for Epirubicin, Doxorubicin, and Methorexate. Zinc and nitrate were shown to be important in the co-assembly, coordinating with drugs and/or Cyclo-HH, thereby enabling drug-peptide as well as drug-drug interactions in successfully formed nanocarriers. The insights could be used in the future design of advanced cancer therapeutic systems with improved properties.

O-nitrobenzyl Caged Molecule Enables Photo-controlled Release of Thiabendazole.

Pesticides are essential in agricultural development. Controlled-release pesticides have attracted great attentions. Base on a principle of spatiotemporal selectivity, we extended the photoremovable protective group (PRPG) into agrochemical agents to achieve controllable release of active ingredients. Herein, we obtained NP-TBZ by covalently linking o-nitrobenzyl (NP) with thiabendazole (TBZ). Compound NP-TBZ can be controlled to release TBZ in dependent to light. The irradiated and unirradiated NP-TBZ showed significant differences on fungicidal activities both in vitro and in vivo. In addition, the irradiated NP-TBZ displayed similar antifungal activities to the directly-used TBZ, indicating a factual applicability in controllable release of TBZ. Furthermore, we explored the action mode and microcosmic variations by SEM analysis, and demonstrated that the irradiated NP-TBZ retained a same action mode with TBZ against mycelia growth.

Influence of Amitraz-Based Product Characteristics on Varroa Mite Population Control

The presence of the Varroa destructor mite requires the use of acaricide treatments for honeybee colonies. Amitraz is one of the most common acaricide-active ingredients used by beekeepers. Certain Varroa mite populations have developed resistance to amitraz, thereby leading to a loss in the efficacy of amitraz-based treatments. Two products, Apivar and Supatraz, were applied in the same apiary in France to evaluate their efficacy. Both treatments are amitraz-based but have different galenics. Thanks to field data, a dynamic model was used to simulate the actions of Apivar and Supatraz on the mite population. We considered two parameters to compare the products as follows: the daily mortality rate and the treatment duration. In the field, the percentage of the efficacy of the two products was not significantly different, but Supatraz kills mites faster and decreases 90% of the mite infestation in 28.4 days compared with 50.9 days when using Apivar. Through modeling, we showed the daily impact of the two different products on mite population. Supatraz has a higher daily mortality rate during the first two weeks than Apivar. Supatraz requires a lower efficacy (% of varroa mites killed during all the treatment) to stabilize the varroa mite population due to its faster release of active ingredients than Apivar, thereby needing a shorter period to achieve the same result. Depending on the model, Supatraz conserves effective efficacy when used against moderately resistant mites (with mite mortality being 40–70% at the LC90) but not against highly resistant mites (with mite mortality being <40% at the LC90). These results show that the comparison of the efficacy of the two products with different characteristics (duration of treatment and daily mortality rate) should be analyzed with caution.

PH/chitinase dual stimuli-responsive essential oil-delivery system based on mesoporous silica nanoparticles for control of rice blast.

Owing to their surface modifiability, smart mesoporous silica nanoparticles (MSNs) can be designed to respond to plant disease-microenvironmental stimuli, thereby achieving on-demand release of active ingredients to control disease by effectively improving citral (CT) stability. A pH/chitinase dual stimuli-responsive essential oil-delivery system (CT@HMS@CH/TA) was successfully fabricated by encapsulating CT in hollow mesoporous silica (HMS), and coating with tannic acid (TA) and chitosan (CH) within HMS by using the layer-by-layer assembly technique (LbL). CT@HMS@CH/TA with an average particle size of 125.12 ± 0.12 nm and a hollow mesoporous nanostructure showed high CT-loading efficiency (16.58% ± 0.17%). The photodegradation rate of CT@HMS@CH/TA under UV irradiation (48 h) was only 15.31%, indicating a 3.34-fold UV stability improvement. CT@HMS@CH/TA exhibited a higher CT release rate in response to acidic pH and the presence of chitinase, simulating the prevailing conditions as Magnaporthe oryzae infection. Furthermore, CT@HMS@CH/TA exhibited better adhesion without affecting normal rice growth, significantly upregulating chitinase gene expression and enhancing chitinase activity on M. oryzae, thus enhancing CT antifungal activity. CT@HMS@CH/TA improved CT stability and showed intelligent, controlled release-performance and higher antifungal efficacy, thus providing a new strategy for efficient application of essential oils for green control of rice blast disease. © 2024 Society of Chemical Industry.

Fluorinated GlycoNucleoLipid-based hydrogels as new spatiotemporal stimulable DDS.

Achieving a controlled release of several active pharmaceutical ingredients (APIs) remains a challenge for improving their therapeutic effects and reduced their side effects. In the current work, stimulable Drug Delivery Systems (DDS) based on supramolecular hydrogels were designed by combining two APIs featuring anticancer activities, namely the doxorubicin and phenazine 14. In vitro studies revealed promising physicochemical properties for all the investigated API loaded gels. Fluorinated GlycoNucleoLipid (GNF) based supramolecular gels remain stable in the presence of either doxorubicin (Doxo) or phenazine 14 (Phe) as anticancer drugs. Noteworthy, the stiffness of the GNF-based supramolecular gels was enhanced in the presence of both APIs while maintaining their thixotropic properties. We demonstrated that the storage modulus (G') of the GNF gels was increased from 1.3kPa to 9.3kPa upon loading of both APIs within the same gels. With a low mechanical stimulation (within the LVR), a passive diffusion out of gels was observed for Dox whereas Phe remained trapped in the GNF gels over several hours. Also, in this work we showed that mechanical stress triggered the release of both Phe and Doxo at different rates.

Microencapsulation for Pharmaceutical Applications: A Review.

In order to improve bioavailability, stability, control release, and target delivery of active pharmaceutical ingredients (APIs), as well as to mask their bitter taste, to increase their efficacy, and to minimize their side effects, a variety of microencapsulation (including nanoencapsulation, particle size <100 nm) technologies have been widely used in the pharmaceutical industry. Commonly used microencapsulation technologies are emulsion, coacervation, extrusion, spray drying, freeze-drying, molecular inclusion, microbubbles and microsponge, fluidized bed coating, supercritical fluid encapsulation, electro spinning/spray, and polymerization. In this review, APIs are categorized by their molecular complexity: small APIs (compounds with low molecular weight, like Aspirin, Ibuprofen, and Cannabidiol), medium APIs (compounds with medium molecular weight like insulin, peptides, and nucleic acids), and living microorganisms (such as probiotics, bacteria, and bacteriophages). This article provides an overview of these microencapsulation technologies including their processes, matrix, and their recent applications in microencapsulation of APIs. Furthermore, the advantages and disadvantages of these common microencapsulation technologies in terms of improving the efficacy of APIs for pharmaceutical treatments are comprehensively analyzed. The objective is to summarize the most recent progresses on microencapsulation of APIs for enhancing their bioavailability, control release, target delivery, masking their bitter taste and stability, and thus increasing their efficacy and minimizing their side effects. At the end, future perspectives on microencapsulation for pharmaceutical applications are highlighted.

Relevance of the Development of Dental &lt;i&gt;In situ&lt;/i&gt; Implant for Post-resection Therapy (Review)

Introduction. The problem of pain relief after surgery is relevant in modern dentistry, as pain control is an important part of treatment. In addition to anesthesia, there are other problems of post-resection therapy such as bleeding from the wound and inflammation. Modern dental practice does not have a targeted delivery system or a medical product with analgesic, anti-inflammatory, anesthetic or hemostatic action, which ensures high adherence of patients to the ongoing post-resection therapy.Text. To solve this problem, it can be proposed to develop an in situ implant – a dosage form that is formed directly at the injection site, in the alveolar socket. Targeted delivery system has advantages: no need to use a medical dressing material; no risk of secondary contamination; dosing accuracy and target delivery to the lesion locus; high mucoadhesion to the site of application; the duration of the active ingredient release and others. The purpose of the review is to substantiate the possibility and relevance of developing a new in situ implant system for use in dental post-resection practice. The study was conducted on the main databases of publications (Scopus, Web of Science, PubMed and others), and patent search database on materials published from 2000 to the present. The study describes the currently existing in situ systems for dental problems, which could be a prototype of systems for delivering an anesthetic directly to the tooth socket, the polymers used to create them and the possibility of releasing drugs, and also characterizes existing drugs for the pain relief (applied both locally and for systemic action), in comparison with in situ systems, which have certain advantages and great potential for development.Conclusion. Based on the results of the work, a conclusion about the possibility of pharmaceutical development of dental in situ implants was made, and the most promising polymers for phase transition in the alveolar socket were identified.

Polydopamine-Doped Porous Nano-CaCO3-Supported Green Tablets for the Humidity-Responsive Intelligent Release of Active Ingredients and Control of Grain Storage Pests

Polydopamine-Doped Porous Nano-CaCO₃-Supported Green Tablets for the Humidity-Responsive Intelligent Release of Active Ingredients and Control of Grain Storage Pests

&lt;i&gt;In-vitro&lt;/i&gt; dissolution profiles comparison for various drugs with active ingredient Febuxostat commercially available on the Russian market

Introduction. Gout treatment drugs are widely represented on the pharmaceutical market of the Russian Federation, including those with INN febuxostat. These drugs differ in excipients composition, in the dosage form (tablets and capsules) and production technology. The Dissolution Kinetics Test was chosen to assess the rate and extent of active ingredient release for drugs with INN febuxostat for different manufacturers as in vitro test dissolution allows to suggest the release from the dosage form in vivo. The rate and percent of active substance release are factors that have a direct impact on the bioavailability of drugs. Drug release was studied in a phosphate buffer solution pH 6.8, sampling was carried out at time points 0 min, 5 min, 10 min, 15 min, 20 min, 30 and 45 min. The analysis of the obtained solutions was carried out using the UV spectrophotometry method at a wavelength of 317 nm. The comparison of dissolution profiles was carried out in accordance with the requirements of Decision of the Council of the Eurasian Economic Commission dated November 3, 2016 N 85 "On approval of the Rules for conducting bioequivalence studies of medicinal products within the framework of the Eurasian Economic Union". The purpose of the study. The purpose of this study was to compare the kinetics of the release of the active substance febuxostat from drugs registered in the territory of the Russian Federation in the form of tablets and capsules. Materials and methods. Drug release studies were performed using the Sotax dissolution tester AT Xtend, Switzerland. Each drug was analyzed in 12 repetitions in a pH 6.8 phosphate buffer dissolution medium, on a "Paddle apparatus", special sinkers were used for capsule dosage forms. The selected samples were analyzed on a Shimadzu UV 1800 UV spectrophotometer, Japan, at a wavelength of 317 nm. Results. Dissolution profile studies for three drugs with the active substance febuxostat were conducted in a phosphate buffer solution pH 6,8. For the studied drugs, the release of febuxostat was observed to be more than 85 % at 15 minutes. The release profiles can be recognized as equivalent without further mathematical processing. Conclusion. Based on the results of dissolution profile studies, no differences were found in dissolution profiles of febuxostat from drugs with different dosage forms (tablets and capsules).

MXene-NH2/chitosan hemostatic sponges for rapid wound healing

Effective control of wound bleeding and sustained promotion of wound healing remain a major challenge for hemostatic materials. In this study, the hemostatic sponge with controllable antibacterial and adjustable continuous promotion of wound healing (CMNCu) was prepared by chitosan, aminated MXene and copper ion. Interestingly, the internal topological point-line-surface interaction endowed the CMN-Cu sponge longitudinal staggered tubular porous microstructure, combined with the lipophilic properties obtained by modified MXene, which greatly improved its flexibility, wet elasticity and blood enrichment capacity. In addition, the sponge achieved controlled release of active ingredients, which made it present highly effective antibacterial activity and long-lasting ability to promote wound healing. In vitro and in vivo experiments confirmed that CMN-Cu sponge presented high-efficient hemostatic performance. Last but not least, a series of cell experiments showed that the CMN-Cu sponge had excellent safety as a hemostatic material.

Burst Release from In Situ Forming PLGA-Based Implants: 12 Effectors and Ways of Correction.

This systematic review examines the reasons for the phenomenon of active ingredient "burst" release, which is a major drawback of PLGA-based in situ formed implants, and the likely ways to correct this phenomenon to improve the quality of in situ formed implants with a poly(DL-lactide-co-glycolide) matrix. Actual and relevant publications in PubMed and Google Scholar databases were studied. The concept of the review was based on the theory developed during literature analysis of 12 effectors on burst release from in situ forming implants based on PLGA. Only those studies that sufficiently fully disclosed one or another component of the theory were included. The analysis resulted in development of a systematic approach called the "12 Factor System", which considers various constant and variable, endogenous and exogenous factors that can influence the nature of 'burst release' of active ingredients from PLGA polymer-based in situ formed implants. These factors include matrix porosity, polymer swelling, LA:GA ratio, PLGA end groups, polymer molecular weight, active ingredient structure, polymer concentration, polymer loading with active ingredients, polymer combination, use of co-solvents, addition of excipients, and change of dissolution conditions. This review also considered different types of kinetics of active ingredient release from in situ formed implants and the possibility of using the "burst release" phenomenon to modify the active ingredient release profile at the site of application of this dosage form.

Hidroxiapatita sustituida con estroncio: plataforma para regeneración ósea con actividad antimicrobiana

Hydroxyapatite (HA) is a calcium phosphate with great analogy to biological apatite. Because of that it has demonstrated excellent results in clinical applications for bone tissue replacement. However, there are certain pathologies such as osteopenia or osteoporosis where the natural bone formation capacity is diminished and which may require an extra stimulus to accelerate and guarantee the osseointegration processes. In these cases, doping hydroxyapatite with strontium ions (Sr-HA) has given excellent results. This ion participates in bone metabolism in various ways and, while stimulating osteosynthesis, it inhibits osteoclast to a certain extent, which as a whole promotes the formation of new bone more quickly. Thus, the development of Sr-HA implants has evolved to not only consider substitutes for bone tissue with greater speed of osseointegration, but also to become platforms for the release of other active ingredients that can also counteract different medical conditions. This work delves into the complexity of septic processes associated with prostheses, which justifies the diversity of approaches to this clinical problem from biomedical engineering. In addition, review different formulations based on Sr-HA reported to eradicate septic processes. In particular, it explores new devices carrying antibiotics (Antb/Sr-HA) and new platforms that have been formed from the double ion doping of the HA where one of those ions is strontium and the other is some metallic element with demonstrated antibacterial activity (M/Sr-HA).

Development of alginate beads for precise environmental release applications: A design of experiment based approach and analysis

Controlled release of active ingredients are important for drug delivery and more recently environmental applications including modulated dosing of chemical and biological controls. This study demonstrates the importance of investigating various material science factors that can influence the diffusion rates of alginate beads to improve and tune their performance for marine environmental applications. This investigation aimed to design a rational workflow to aid in leveraging alginate bead use as a carrier matrix for releasing a specific active agent into water. Experiments were conducted to focus on the narrow a large list of relevant material formulation parameters, which included chitosan molecular weight, chitosan concentration, calcium concentration, drop height, and bead size. Once the most relevant material preparation methods were screened, a more robust statistic Design of Experiments approach was performed and results determined the important (and unimportant) factors for increasing dye release kinetics in marine water. The process was further streamlined by narrowing the critical experimental factors to a three-level based on the prior analysis: chitosan MW, chitosan concentration, and bead size. Analysis of the collected data indicated that while chitosan MW had a negligible impact (Fstatistic = 0.22), bead size (Fstatistic = 60.33) significantly influenced the diffusion rates based on surface area. However, chitosan MW had minor effects where lower chitosan MW enabled higher product release rates. This case investigation was a novel application of the design of experiment approach towards environmental applications to understand differences in release rates to marine waters for the first time and the workflow provided also serve as the basis for researchers to optimize other environmental applications requiring optimization when it is unknown how a large number of formulation variables will impact performance in different environmental scenarios.

Near infra-red absorbing Quinolizidine fused curcuminoid-BF2 chelate and its applications in photodynamic therapy using MCF-7 and A549 cells

Metal-free near-infrared absorbing photosensitizers (PS) have been considered promising candidates for photodynamic therapy. Curcumin, curcuminoid, and its derivatives have therapeutic values due to their anti-inflammatory, antifungal, and antiproliferative properties. Curcuminoid-BF2 chelates have also been studied as cell imaging probes, however, their applications in photodynamic therapy are rare. In this article, we describe the synthesis and therapeutic evaluation of quinolizidine fused curcuminoid-BF2 chelate (Quinolizidine CUR-BF2) containing an acid-sensitive group. This donor-acceptor-donor curcuminoid-BF2 derivative exhibits absorption and emission in the deep red region with an absorption band maximum of ∼647 nm and a weak emission band at approximately 713 nm. It is interesting to note that this derivative has a high molar extinction coefficient (164,655 M−1cm−1). Quinolizidine CUR-BF2 possesses intramolecular charge transfer properties, facilitating the production of singlet oxygen (1O2), which plays a crucial role in cell death. Additionally, Quinolizidine CUR-BF2 can enable the selective release of active ingredients in an acidic medium (pH 5). Furthermore, the nanoaggregates of PS were prepared by encapsulating Quinolizidine CUR-BF2 within Pluronic F127 block co-polymer for better water-dispersibility and enhanced cellular uptake. Dark cytotoxicity of nanoaggregates was found to be negligible, whereas they exhibited significant photoinduced cytotoxicity towards cancer cells (MCF-7 and A549) under irradiation of 635 nm light. Further, the cell death pathway using Quinolizidine CUR-BF2 nanoaggregates as PS is found to occur through apoptosis. Specifically, the present study deals with the successful preparation of Quinolizidine CUR-BF2 nanoaggregates for enhanced water-dispersibility and cellular uptake as well as the efficacy evaluation of developed nanoaggregates for photodynamic therapy.