Indonesian Journal of Pharmacy

Nano-Enabled Phytotherapeutics for Obesity Management: Translating Preclinical Discoveries into Clinical Opportunities

2026-05-11T13:24:52+07:00

Obesity represents a major global public health challenge associated with long-term complications such as type 2 diabetes, cancer, cardiovascular diseases, and respiratory disorders, largely driven by modern lifestyles and unhealthy dietary patterns. Although conventional treatment strategies, including lifestyle modification, pharmacotherapy, and bariatric surgery, offer therapeutic benefits, they are often limited by adverse effects, long-term adherence, and inconsistent efficacy. In recent years, herbal medicines and phytoconstituents have emerged as attractive alternatives due to their natural origin, multitargeted mechanisms of action, and comparatively favorable safety profiles. However, their clinical translation is frequently hampered by poor aqueous solubility, low bioavailability, and rapid systemic clearance. Nanotechnology provides a promising approach to overcome these limitations by improving the pharmacokinetics, stability, and targeted delivery of bioactives. This review presents a comprehensive evaluation of herbal nanotherapeutics for obesity management, focusing on the design and application of diverse nanocarrier systems, including polymeric nanoparticles, nanoemulsions, liposomes, solid lipid nanoparticles, and micelles. Additionally, current challenges, regulatory considerations, and future perspectives are examined to guide the development of safe, effective, and patient-friendly herbal nanomedicines for obesity treatment.

Advancements in Cubosomes: A Promising Platform for Targeted Anticancer Drug Delivery

2026-05-11T13:25:54+07:00

Nanosized particles are stabilised by polymers and made mostly of amphiphilic lipids known as cubosomes (CUBs). Encapsulating hydrophilic, hydrophobic, and amphiphilic pharmaceuticals is made effective by their internal bi-continuous cubic phase architecture, which gives a high surface area and partitioned aqueous domains. These self-assembled nanoparticles exhibit thermodynamic stability, biocompatibility, and mucoadhesive properties, making them ideal carriers for diverse multiple administration routes, including oral, transdermal, parenteral, and ocular. Problems with medication solubility, bioavailability, and non-specific toxicity are some of the most important ones that CUBs aim to solve. This review presents a comprehensive overview of CUB structure, types, formulation methods, and characterization techniques. The review emphasizes recent advancements in CUB-based delivery of chemotherapeutic agents, including paclitaxel and doxorubicin, cisplatin, methotrexate, and 5-fluorouracil, highlighting their improved pharmacokinetics and reduced systemic toxicity Despite manufacturing challenges, ongoing research into scalable production and novel excipients continues to support their translational promise. CUBs represent a versatile and potent platform in nanomedicine, offering substantial improvements in drug delivery and cancer treatment. Recent advancements in formulation strategies and surface modification is further strengthened their therapeutic potential. Cubosomes as a promising platform in precision oncology and next generation cancer therapeutics.

Recent Trends in Electrospun Nanofibers for Drug Delivery Systems in Asia

2026-05-07T11:22:06+07:00

Electrospun nanofibers have gained increasing attention as an advanced platform for drug delivery due to their high surface-area-to-volume ratio, tunable porosity, and ability to incorporate a wide range of therapeutic agents. These structural properties enable precise control over drug loading and release kinetics, making electrospun nanofibers a promising alternative to conventional delivery systems such as liposomes, hydrogels, micelles, and polymeric nanoparticles. This review provides a comprehensive overview of electrospinning fundamentals, polymer–solvent interactions, and key processing parameters influencing nanofiber morphology and performance. Various drug encapsulation strategies, including blend, coaxial, and emulsion electrospinning, are discussed together with their advantages and limitations in achieving controlled and stimuli-responsive drug release. A narrative literature search covering the period 2015–2025 identified 214 studies, of which 137 met the eligibility criteria and were included in this review. The findings reveal significant research progress across several Asian countries, particularly China, Japan, South Korea, India, and Malaysia, where electrospun nanofibers are actively explored for applications in cancer therapy, wound healing, topical drug delivery, and tissue engineering. The integration of natural bioactive compounds, implantable nanofiber systems, and stimuli-responsive architectures further highlights the rapid innovation occurring in this region. Despite these advancements, several challenges remain, including high production costs, limitations in large-scale manufacturing, solvent toxicity, environmental concerns, and the lack of standardized regulatory frameworks. Addressing these issues through improved fabrication technologies, modular electrospinning systems, solvent recycling strategies, and harmonized quality standards will be essential for successful commercial translation. Overall, electrospun nanofibers represent a rapidly evolving and highly adaptable platform with strong potential to advance future drug delivery strategies, particularly within Asia’s growing pharmaceutical and biomedical landscape.

Development and Optimization of Technetium-99m Radiolabeled Chitosan Nanoparticles for Potential Theranostic Applications in Cancer

2026-05-08T11:09:12+07:00

The appealing physical properties of ^99mTc, such as its 6-hour half-life, emission of 140 keV gamma rays, and availability from affordable generators, have made its application preferable in SPECT imaging. The labelling of certain targeting moieties such as nanoparticles with ^99mTc could improve the detection of diseased tissues for enhanced diagnosis and therapies. Chitosan nanoparticles which possess many appealing properties like biocompatibility and biodegradability, have been the focus of many scientific studies, demonstrating its use in various applications. In this study, chitosan nanoparticles were developed using the ionic gelation method, and the effect of concentration and pH of the medium on the size of the nanoparticles were evaluated. The nanoparticles produced were radiolabelled with ^99mTc, which has a radioactivity range of between 100–111 MBq (2.7–3 mCi), and the stability of the radiolabelling was evaluated. The nanoparticles were found to be in the nanometres range, between 81 to 270 nm. The labeling efficiency of the ^99mTc-labeled chitosan nanoparticles was determined to be higher than 90%, with more than 6 hours of stability. In conclusion, the ^99mTc-radiolabelled chitosan-based radiopharmaceutical has shown good and promising characteristics and may be potentially useful as a dual-function theranostic agent in the future.

Redox-Driven Stability and Synergism of Glabridin and Proanthocyanidin Nanoparticles

2026-05-08T11:08:25+07:00

This study aimed to develop and characterize phosphatidylcholine-based nanoparticles encapsulating proanthocyanidin and glabridin, two natural polyphenolic antioxidants. Nanoparticles were prepared by the solvent-displacement method and characterized for particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency, and in vitro release. Antioxidant activity was evaluated using DPPH, ABTS, and FRAP assays, and physical and chemical stability was assessed during storage at 4°C and 30°C for four weeks. The optimized glabridin and proanthocyanidin nanoparticles exhibited mean sizes of 85.42 ± 3.29 nm and 159.47 ± 4.47 nm, with encapsulation efficiencies of 49.73 ± 0.72% and 89.48 ± 4.57%, respectively. Both formulations demonstrated a biphasic release profile and enhanced antioxidant activity compared to their free forms. Notably, the 2:1 glabridin-to-proanthocyanidin nanoparticle combination exhibited the highest ferric-reducing antioxidant power (FRAP), suggesting potential for redox regeneration and synergistic interactions. Stability studies revealed that 4°C storage effectively preserved particle integrity, antioxidant activity, and compound content, whereas 30°C accelerated degradation and reduced scavenging capacity. These findings suggest that nanoencapsulation not only improves the solubility and stability of poorly water-soluble antioxidants but may also enhance antioxidant efficacy via redox cycling and favourable partitioning within the nanoparticle matrix. This dual-antioxidant nanoparticle system holds promise for oxidative stress mitigation.

Development, Optimization, and Physicochemical Characterization of Liposomal Formulations Containing Ethanolic Leaf Extract and Flavonoid-Rich Fraction of Albizia lebbeck for Enhanced Hepatoprotective Delivery

2026-05-08T11:13:02+07:00

This work describes the development, optimization and characterization of liposomal carriers loaded with an ethanolic leave extract and a flavonoid-rich fraction of Albizia lebbeck (A. lebbeck) to improve hepatoprotective activity. Liposomes were prepared by the thin film hydration method, followed by probe sonication and optimized for vesicle size, zeta potential, PDI, and encapsulation efficiency. The ethanolic extract-loaded liposomes exhibited a smaller vesicle size of 152.4 ± 3.6 nm, a polydispersity index of 0.212 ± 0.01, a zeta potential of −32.6 ± 2.3 mV, and an encapsulation efficiency of 67.8 ± 2.4%. On the other hand, the liposomes encapsulating flavonoid-rich fraction resulted in a smaller vesicle size (138.2 ± 4.1 nm), a lower PDI (0.198 ± 0.02), a more negative zeta potential (−36.2 ± 1.9 mV), and a significantly higher encapsulation efficiency (82.5 ± 1.7%). Morphological characterization by Transmission Electron Microscopy (TEM) showed consistently spherical vesicles. In vitro release studies revealed even a better controlled release profile over 24h, where flavonoid-loaded liposomes released 82.3% compared to 30.1% released from the crude extract-loaded liposomes after 24h. The physical stability of the liposomal formulations was improved, as evidenced by stability studies conducted at 4°C and 25°C for 30 days. Thus, these results suggest that the bioavailability, stability and therapeutic effects of A. lebbeck components, particularly the flavonoid-rich fraction, can be significantly improved by liposomal encapsulation, thus supporting its potential application as an advanced hepatoprotective delivery system.

Gnetum gnemon L. Seed Hardshell Nanoextract, A Potential Biomaterial for Oral AntiAging through Sirtuin-1 Activation

2026-05-11T13:00:09+07:00

The seeds of Gnetum gnemon L. widely referred to as melinjo, enclosed within a distinctly tough outer shell, have attracted interest due to their remarkable anti-aging capabilities. Nevertheless, despite this potential, their practical therapeutic use is limited by their naturally low solubility and restricted bioavailability. To tackle these pharmacokinetic issues, the current study utilized an environmentally friendly nanotechnology approach, specifically high-energy ball milling, to create nanoparticles from the hard shell of the seeds. This technique significantly amplifies the surface area of the bioactive particles, thus improving their absorption and efficacy within biological systems. The resulting nanoextracts were comprehensively characterized and subsequently assessed through in vivo anti-aging tests and acute oral toxicity evaluations. UVB-irradiated rats served as a biological model for simulating aging, with nanoextracts administered at doses of 36, 72, and 144 mg/kg over a duration of 12 weeks. The results demonstrated a statistically significant, dose-dependent rise in the expression of SIRT1, a crucial regulatory protein associated with cellular longevity and aging mechanisms. Notably, an acute toxicity evaluation at a dosage of 5000 mg/kg affirmed the safety of the nanoformulation, with no discernible toxic effects noted in the test subjects. These results highlight the promise of G. gnemon seed hardshell nanoparticles as a feasible and safe natural alternative for anti-aging therapies. The implementation of sustainable nanotechnology not only enhances the delivery and effectiveness of phytochemicals but also corresponds with the increasing demand for environmentally friendly biomedical advancements aimed at fostering healthy aging.

Application of D-Optimal Mixture Design to Optimization and Formulation of Erythropoietin in Nanoparticles Drug Delivery System

2026-05-07T11:12:48+07:00

Erythropoietin (EPO) is a glycoprotein hormone used to treat anemia in patients with chronic renal failure in an injection dosage form. Drug delivery systems with nanoparticles technology have a high potential in increasing protein stability, prolonging the duration of the therapeutic effect, and the application without injection. This study aims to optimize the formulation of erythropoietin nanoparticle oral preparation using the D-optimal mixture design. This study is to determine the concentration range of chitosan and pectin as a base for nanoparticles. The D-optimal mixture design optimizes the erythropoietin nanoparticles by selecting the nanoparticle base composition as an independent factor and nanoparticle characterization as a response. Nanoparticles in the optimal formula were characterized, including particles size, polydispersity index (PDI), zeta potential, and encapsulation efficiency. The data were analyzed by using ANOVA contained in the Design Expert® software to get the optimum formula. The optimization showed that the optimal formula was that using 0,10% chitosan and 0,010% of pectin. Nanoparticle loaded erythropoietin produced with 278,8 nm of particle size, 0,38 of PDI, 27,0 mV of zeta potential, and 87,32% entrapment efficiency. In this study of the D-optimal mixture design, and optimize and prepare the erythropoietin nanoparticles

Development of Orodispersible Film Containing Spray-Dried Rifampicin Nanosuspension

2026-05-08T08:35:22+07:00

Tuberculosis (TB) is a major global health challenge, with high mortality rates. Conventional anti-TB dosage forms, such as tablets are often unsuitable for patients who struggle with swallowing, leading to poor
compliance. Therefore, this study aimed to develop orodispersible film (ODF) containing rifampicin, a widely used anti-TB drug. Rifampicin’s low aqueous solubility poses challenges for its incorporation into ODF and
affects its therapeutic effectiveness. To address these issues, rifampicin was first prepared as nanosuspension and subsequently dried before being formulated into ODF. Nanosuspension was stabilized using polyvinyl alcohol (PVA), poloxamer 188 (POX), and the combination at various concentrations. Nanosuspension was prepared using solvent-antisolvent precipitation followed by sonication and spray-drying. Spray-dried nanosuspension was characterized, and the optimal formula was used in ODF formulation through the solvent-casting method. Formulations PV2 (PVA 0.4%) and POX1 (POX 0.2%) showed the smallest particle sizes at 306±14.01 nm and 291±7.55 nm, respectively. After reconstitution, PV2 maintained particle size comparably to POX1. Spray-dried PV2 nanosuspension exhibited a 21.48-fold increase in saturated solubility compared to the pure rifampicin, and showed superior drug release, with 79% release versus 58% for the standard rifampicin suspension. ODF containing PV2 showed improved organoleptic properties and enhanced drug dissolution (82% vs 56%) compared to original rifampicin ODF. The formulation of rifampicin into nanosuspension stabilized by PVA and POX, followed by spray-drying, significantly improved solubility and drug release profile. This method also enhanced the organoleptic properties and dissolution of rifampicin in ODF, providing a promising strategy to boost rifampicin’s therapeutic efficacy in TB treatment, particularly for pediatric patients.

Liposomal Formulation of Plant Based Natural Photosensitisers for Thrombosis

2026-05-07T08:39:25+07:00

Photothermal and photodynamic therapy (PTPDT) in medical field continue to evolve due to their relatively low adverse effect and high efficiency for therapeutic application. Photosensitisers compounds have shown excellent ability in inducing mild hyperthermia and generation of reactive oxygen species (ROS) which is beneficial for thrombolysis. Herein, we explored plant-based sources rich in pigments such as beet root (BR), butterfly pea flower (BPF), red cabbage (RC), purple sweet potato (PSP) and phycocyanin (PHY) as natural photosensitisers (NPS) candidates for the treatment of thrombosis. We were able to produce extracts with strong absorption within the 400-800 nm wavelength range, the ideal window for photosensitisation. The photosensitising ability of the NPS were confirmed after significant photothermal increase was achieved after 5 minutes low intensity exposure with 450 nm and 550 nm lasers. Extract from BPF, RC, BR and PHY were the most promising and further formulated into liposomes. Through in vitro thrombolytic activity on human blood clots, we confirmed thrombolytic capability of NPS comparable to that of nattokinase. Liposomal formulation of the best NPS (Lip-PHY and Lip-BPF) produced particles of ~168.3 and 215.9 nm respectively, with good encapsulation efficiency and stability. Ultimately with this study, we have demonstrated liposomal formulation of NPs and their strong potential as thrombolytic agent.

In Vivo Antihyperglycemic Study of Insulin Self-Nanoemulsifying Drug Delivery System (SNEDDS)

2026-05-08T14:43:50+07:00

To deliver insulin orally requires an appropriate formulation strategy. Self nano-emulsifying drug delivery system (SNEDDS) can be used as an alternative to increase insulin bioavailability and activity. This study aim was to evaluate the antihyperglycemic activity of SNEDDS insulin. Insulin was loaded in SNEDDS by first dissolving it in glycerin. The dissolved content in glycerine was determined spectroscopically using the Bradford method. Insulin SNEDDS is then administered orally in rats in a variety of doses such as 43.39; 108,47; 216.94 IU / Kg. The rats used in this study were diabetic rats that had been induced with streptozotocin 48 mg / Kg BW. The insulin SNEDDS given can reduce blood glucose levels, while insulin without SNEDDS, PBS pH 7.4, and blank SNEDDS cannot lower blood glucose levels. The results of this study indicate that insulin given using the SNEDDS formulation can increase insulin activity, which is entirely ineffective if given orally without SNEDDS formulation.

Keywords: Insulin, SNEDDS, Oral, Antihiperglycemic

Study of Formyl and Phenyl Substituted Styrylpyrazolines: Synthesis, In Vitro Antibacterial Evaluation¸ and Molecular Docking against DNA Gyrase

2026-05-07T08:39:25+07:00

Bacterial resistance to most antibiotics remains a persistent challenge, urging the need for the development of novel antibacterial agents. Styrylpyrazoline derivatives have shown diverse biological activity, including as an antibacterial. This study synthesized and evaluated styrypyrazolines 2a and 2b for their antibacterial activity against Gram-positive and Gram-negative bacteria (Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa). The in vitro evaluation was performed using disc diffusion and microdilution methods. The result revealed that both compounds have the highest inhibition against S. aureus. Moreover, the presence of formyl group (-CHO) on styrylpyrazoline 2a enhanced its inhibitory activity against P. aeruginosa. Neither compound showed significant inhibition against B. subtilis or S. epidermidis. Molecular docking of both compounds against DNA gyrase subunit B was performed to further investigate their antibacterial mechanism. It was revealed that both compounds are able to interact with the receptor within the ATP-binding pocket. Similar to ciprofloxacin, compound 2a formed hydrogen bonds with the Asp81 residue, showing its potential as a DNA gyrase inhibitor. While compound 2b formed aromatic-hydrogen bridging with Pro87 residue. This study suggests that styrypyrazolines 2a and 2b possess promising antibacterial activity. However, their potency is lower than the reference drug. Thus, further modification of the structure is necessary to enhance their potency as antibacterial agents.

Keywords: styrylpyrazoline, antibacterial, DNA gyrase, docking

Discovery of New Amphipathic Helix Antibacterial Peptides with Proteomic Analysis using LC-HRMS and Virtual Screening

2026-05-08T13:21:15+07:00

Antimicrobial peptide is an alternative to combat antibiotic resistance with typical characteristics such as amphipathic and helical structure. Several approaches such as virtual and conventional screening have been employed to discover new antibacterial peptides. In the current study we aim to discover new antibacterial peptides with virtual screening by filtering proteomic data bank of Chondrus crispus using machine learning. The proteomic data bank of Chondrus crispus were generated by LC-HRMS after tryptic digestion. The candidate peptides selection was carried out using machine learning and AMP’s characteristics. The proteomic study resulted 3645 candidate peptides. The first filtering using a positive charge characteristic, avoid amino acid and 12 – 50 residual lengths resulted 175 candidate peptides. Twelve candidate peptides were resulted second filtering by scoring using CAMPR4 and dbAMP. The last filtering performed by physicochemical analysis resulted three selected peptides CC1 (FSTSSRALRFFR), CC2 (RDLQQAISMVKK), and CC3 (IAAKIQLLRSYR). All selected peptides have promising physicochemical with amphipathic structures. The secondary structure analysis by CD showed that all peptides have a random coil structure in water and helix structure in 50% TFE. CC1 and CC3 showed inhibitions up to 100% at 250 μg/mL concentration against E. coli. However, both peptides exhibited lower activity against S. aureus with inhibitions around 50-60% at 250 μg/mL.

Dipeptidyl Peptidase 4 Inhibitory Activity of Protein Hydrolysate from Earthworms (Perionyx excavatus)

2026-05-08T13:40:30+07:00

Diabetes is a complex metabolic syndrome, of which type 2 diabetes (T2DM), primarily caused by impaired insulin response, accounts for 95% of diabetes cases worldwide as of 2021. One treatment strategy to control T2DM includes inhibiting dipeptidyl peptidase-4 (DPP4), an enzyme that breaks down incretin hormones and impairs glucose regulation. This study explores the potential of hydrolysed proteins from earthworms (Perionyx excavatus) as natural DPP4 inhibitors, focusing on optimizing hydrolysis conditions, including enzyme type hydrolysis, earthworms:phosphate buffer (w/v), temperature (°C), pH, enzyme:substrate (E:S) ratio (U/g protein), and time hydrolysis (hour). Among the tested enzymes, Alcalase produced the most effective hydrolysate. The optimal conditions for hydrolysis were determined at an E:S ratio of 1:6 (w/v), a temperature of 55°C, pH 7, an enzyme: substrate ratio of 600 U/g protein, and a hydrolysis time of 4 hours. Under these conditions, the resulting hydrolysate exhibited vigorous DPP4 inhibitory activity (DPP4IA), with an IC₅₀ value of 777.18 μg/mL. Further ultrafiltration fractionation revealed that the <1 kDa fraction had the highest inhibitory activity, with IC₅₀ values of 395.03 and 323.07 μg/mL before and after digestion, respectively. Notably, the hydrolysate demonstrated stability across a broad pH range (1–11) and remained bioactive even after exposure to 100°C for up to 180 minutes. Interestingly, enzymatic hydrolysis and simulated digestion appeared to enhance bioactivity, likely due to the generation of smaller bioactive peptides. These findings suggest that peptides derived from Perionyx excavatus could be promising natural DPP4 inhibitors with potential applications in functional foods or pharmaceutical formulations for blood glucose management.

Vancomycin-Loaded Nano Bovine Hydroxyapatite-Poly(lactic-co-glycolic acid)-Polyethylene Glycol Nanofibers for Controlled Drug Delivery: Design, Characterization, and Kinetic Modeling

2026-05-08T08:02:50+07:00

Bone fractures and orthopedic surgical interventions are associated with an increased risk of osteomyelitis, necessitating effective antibiotic therapy. However, systemic antibiotic administration is often limited by poor drug penetration due to tissue devascularization at the fracture site and the formation of bacterial biofilms, which further contribute to antimicrobial resistance and systemic toxicity. Consequently, localized drug delivery systems have emerged as a promising strategy to overcome these limitations. This study aimed to fabricate vancomycin (VAN)-loaded nanofiber implants based on a nano bovine hydroxyapatite (NBHA)–poly(lactic-co-glycolic acid) (PLGA)–polyethylene glycol (PEG) matrix with optimized physicochemical properties and a sustained release profile over 28 days. The nanofibers were fabricated via electrospinning using an optimized formulation derived from a prior Design of Experiments (DoE) study. The resulting nanofibers exhibited uniform morphology, with an average fiber diameter of 91.42± 0.85 nm and a tensile strength of 2.152±0.289 MPa, indicating suitable mechanical properties. In vitro release studies demonstrated a sustained release profile with a dissolution efficiency of 67.74% over 28 days. The release kinetics were best described by the Peppas–Sahlin model during the initial phase and transitioned to the Higuchi model at later stages, suggesting a combination of diffusion- and polymer relaxation-controlled mechanisms. Overall, VAN-loaded NBHA–PLGA–PEG nanofiber implants demonstrate significant potential as a localized and controlled drug delivery platform for osteomyelitis therapy while concurrently supporting bone regeneration.