Journal of Pharmaceutical Innovation最新文献

Purpose

The purpose of this study was to formulate and investigate biopolymer based cryogel as bioactive carriers, which is hydrophilic in nature.

Methods

A Contemporary research based on the preparation of hemoglobin protein-polyvinyl (Hb-PVA) macroporous cryogels of varying compositions through the freeze–thaw method, using deionized water as a plasticizer. Vancomycin drug loaded Hb-PVA gel applicable as a good platform to promote controlled antibiotic drug release into the specific sites of the body against antibiotic resistance diseases.

Results

The synthesized Hb-PVA cryogels were characterized by spectroscopic and microscopic techniques such as Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD). Additionally, the morphological and thermal stability of the synthesized cryogels were studied by scanning electron microscopy (SEM) and differential scanning calorimetry. FTIR and XRD spectral assignments revealed the crystalline nature of the cryogel with semicrystalline segments. In addition, scanning electron microscopy (SEM) images revealed that the surface morphology was macroporous in nature; hence, the water-holding capacity of these materials increased. Atomic force microscopy images reveal that the surface roughness is enough for the adhesion of drug molecules, and the R_a/R_q ratio is equal to 1.24 for a Gaussian surface. The swelling properties of the prepared cryogels were investigated at different polymer compositions, temperatures, simulated biological solutions, pH media, salt solutions, and freeze thaw cycles at certain time intervals. The swollen gels were further investigated for vancomycin drug loading and release profiles under in vitro conditions, such as changes in the polymer (PVA, Hb) concentration, temperature, and pH of the release media. This drug-loaded cryogel was also examined for its antibacterial activity against gram-positive and gram-negative bacteria.

Conclusions

The protein based cryogels have great potential to deliver antibiotic drugs or other bioactive compounds. Based ontheir pore-sizes they may also use in water treatment and cell proliferation, wound dressing etc.

Purpose

Ondansetron (OND) is 5-HT3 receptor antagonist commonly used to treat chemotherapy-induced nausea and vomiting. However, its short half-life, low bioavailability, and intense bitter taste have led to decreased patient compliance. Administering it via an oromucosal film encapsulated into polymeric nanoparticles without the need for water is advantageous due to the difficulty of taking the medication with water when experiencing nausea. Therefore, the aim of this study was to synthesise polymeric nanoparticles using L-cysteine amino acid to encapsulate the bitter-tasting OND and develop paediatric oral dissolving films (ODFs) using them.

Method

Cysteine-based poly(amide-thioester) nanoparticles (CYS-PATE NPs) were developed using the one-step interfacial polycondensation technique between aqueous and organic phases. The nanoparticles were extensively characterised and incorporated into ODFs prepared using various polymers (HPMC, Pullulan and Polyethylene oxide (PEO)).

Results

OND-loaded CYS-PATE NPs (OND/CYS-PATE NPs) were also synthesised with a particle size of 319.7 ± 44.59 nm and a zeta potential of -32.07 ± 0.31. The semi-crystalline nature of both the resultant CYS-PATE NPs and the OND-encapsulated ones was confirmed by DSC and XRD characterisation. In-vitro release studies of optimal formulation (OND/CYS-PATE NPs) showed a total release of 58 µg of OND in 10 mL of artificial saliva after 10 min, equivalent to 5.8 µg/mL, which did not reach the OND bitterness threshold (7.5 µg/mL). Incorporating these NPs into film-forming polymers led to the development of 0.1% HPMC ODFs with homogeneity and a good disintegration time of 49.33 ± 3.99 s.

Conclusions

This study confirms that encapsulating bitter actives in CYS-PATE NPs effectively masked the taste of bitter soluble APIs, formulating them into more palatable forms that can enhance acceptability and adherence, particularly in paediatrics CINV.

Graphical Abstract

Schematic representation diagram of synthesis and characterisation of L-cysteine amino acid based poly (thioester amide) nanoparticles containing OND for taste masking of it

Purpose

Conventional cancer treatments often possess systemic side effects, limiting their efficacy. Nanosponges present a promising solution for targeted drug delivery, allowing precise release of encapsulated drugs and enhanced bioavailability.

Methods

Using a statistical design approach (Box- Behnken design), the nanosponges were optimized to achieve controlled particle size and drug % EE. The optimized formulation (DZ-NS 4) was incorporated into a hydrogel base using HPMC to enable controlled drug delivery. In-vitro, in-vivo, and ex-vivo characterisations were performed to assess drug release, skin permeation and biocompatibility.

Results

The optimized DZ nanosponges showed controlled particle size (338.6 nm) and high entrapment efficiency (92.2%). Subsequent in-vitro characterization of DZ nanosponge hydrogel demonstrated sustained drug release (82% over 12 h), and ex-vivo showed effective skin permeation (73% through sheep skin), and good in-vivo biocompatibility showing minimal signs of skin reactions. The optimized formulation exhibited substantial anti-proliferative activity, with an IC₅₀ value of 68.81 µg/mL, compared to the standard cisplatin, which had an IC₅₀ value of 6022.0 µg/mL, indicating superior inhibition of melanoma cell proliferation.

Conclusion-

Taken together, this study successfully designed a novel Dacarbazine nanosponges hydrogel with promising topical therapeutic option for Melanoma treatment, offering targeted delivery, sustained therapeutic effects, and minimal systemic side effects.

Graphical Abstract

The emergence of antifungal resistance and suboptimal drug delivery systems presents a significant challenge in treating dermatophytosis, necessitating innovative therapeutic approaches. Here, we report the development of an advanced drug delivery platform utilizing electrospun nanofibers incorporating bisabolol, demonstrating superior antifungal efficacy and controlled release properties. Through systematic optimization of polymer compositions, we engineered nanofiber networks using precise combinations of polycaprolactone (PCL), polyvinylpyrrolidone (PVP), and gelatin, incorporating bisabolol at a carefully calibrated 5% w/w drug-to-polymer ratio. Comprehensive morphological characterization via scanning electron microscopy revealed that bisabolol incorporation significantly enhanced fiber uniformity and reduced diameter distributions, with the optimized PCL100/PVP80 formulation exhibiting exceptional structural integrity. This formulation demonstrated remarkable antifungal activity, producing substantial inhibition zones against clinically relevant dermatophytes: Trichophyton mentagrophytes (2.05–2.6 cm, p < 0.001), Trichophyton tonsurans (2.5 cm, p < 0.001), and Alternaria alternata (1.04 cm, p < 0.01). High-performance liquid chromatography analysis confirmed sustained drug release kinetics over 48 h, maintaining therapeutic concentrations throughout the treatment period. Cytotoxicity evaluation through MTT assays revealed outstanding biocompatibility, with the PCL100/PVP80-bisabolol formulation maintaining 81.92 ± 4.33% fibroblast viability, significantly superior to conventional formulations (p < 0.001). This study presents a paradigm shift in topical antifungal therapy, offering a precisely engineered, biocompatible platform that addresses current therapeutic limitations. The developed system’s demonstrated efficacy, controlled release properties, and excellent safety profile position it as a promising candidate for clinical translation in treating chronic dermatophytosis, particularly in cases resistant to conventional treatments.

Graphical Abstract

Background

The present study aimed to design and develop aprepitant-loaded self-microemulsifying drug delivery systems (SMEDDS) and to characterize and assess their intestinal permeability.

Methods

D-optimal design has been used to design and optimize the ratio of formulation components. Prepared aprepitant-loaded SMEDDS formulations were subjected to in vitro characterization studies. Single pass intestinal perfusion method (SPIP) was applied to evaluate the intestinal permeation of aprepitant-loaded SMEDDS and compare it with free aprepitant.

Results

The optimum level of formulation components was determined as oleic acid 10%, Tween 80 60%, and Transcutol P 30%. The particle size of aprepitant-loaded SMEDDS was 152 nm and its PDI (polydispersity index) was 0.35. The optimized aprepitant-loaded SMEDDS showed a zeta potential of -21 ± 8. Effective intestinal permeability (P_eff) of free aprepitant was 1.27 ± 0.44 × 10^− 4 cm/s, whereas for the optimized aprepitant-loaded SMEDDS formulation, it was 2.61 ± 0.79 × 10^− 4 cm/s.

Conclusion

SMEDDS could be considered a promising delivery system for increasing oral bioavailability of aprepitant as the optimized aprepitant-loaded SMEDDS formulation revealed appropriate physicochemical properties and significantly enhanced intestinal permeability.

Purpose

Bioprospect a polymeric film containing P. cauliflora extract (PCE) for the differential treatment of skin injuries.

Methods

Films containing 1%, 3% and 5% of PCE were prepared and subjected to physicochemical characterization, including thickness measurement, mechanical and barrier property analysis, colorimetric evaluation, FTIR, release profiles and antimicrobial properties. Additionally, in vivo wound healing efficacy was evaluated over 21 days.

Results

The films displayed uniform thickness and high malleability. Incorporating PCE improved water solubility, reduced water vapor permeability rate and moisture absorption capacity. The bioactive release was sustained for over 24 h, ensuring an extended therapeutic window. These properties make them ideal for topical applications by providing a structured matrix for controlled bioactive release upon wound contact. This design maintains a moist environment, prevents adherence to the wound, and minimizes common issues associated with traditional treatments, such as tissue trauma during dressing changes. Antimicrobial analysis confirmed the inhibitory activity against Staphylococcus aureus in films loaded with 3% and 5% PCE. In vivo studies demonstrated accelerated wound healing with a film loaded with 5% PCE.

Conclusion

The films loaded with 5% PCE demonstrated optimal therapeutic efficacy by promoting wound healing and providing sustained antimicrobial activity, thereby serving as a viable alternative to conventional films. These films offer a structured bioactive matrix with controlled release. Unlike conventional treatments such as ointments, they offer a promising and innovative approach for skin injury treatment.

Purpose

Chinese medicine polysaccharide are considered as promising medical materials due to their good biocompatibility and safety. The aim of this study was to develop a novel amphiphilic drug carrier based on astragalus polysaccharide (APS) to optimise the delivery of paclitaxel.

Methods

The pH-sensitive histidine (His) and hydrophobic stearic acid (SA) were grafted onto astragalus polysaccharide and self-assembled into nanoparticles by ultrasonication. The nanoparticles were characterised by Fourier transform infrared (FTIR), dynamic light scattering (DLS), zeta potential, transmission electron microscopy (TEM), and X-ray diffraction, and tested for encapsulation efficiency (EE%), drug loading capacity(LC%) and in vitro release of paclitaxel. The effects of nanoparticles on the proliferation of immune cells RAW264.7 and breast cancer cells SUM149 were assessed by cck-8 assay, and their effects on SUM149 cell cycle block and apoptotic protein expression were detected.

Results

The EE% of nanoparticles on paclitaxel was 77.61% and the LC% was 9.96%. Under acidic conditions, the surface charge of nanoparticles was reversed and the structure was swollen to promote drug release. Cellular experiments showed that blank nanoparticles could promote the proliferation of immune cells, and the anticancer effect of drug-loaded nanoparticles was significantly better than that of paclitaxel alone.

Conclusion

The prepared pH-sensitive nanoparticles can effectively enhance the uptake of paclitaxel by tumour cells and induce apoptosis in breast cancer cells, making them a promising new type of paclitaxel drug carrier.

Purpose

Three-dimensional (3D) printing is revolutionising tablet fabrication in the field of pharmacy, offering personalised dosing through additive manufacturing techniques such as semi-solid extrusion (SSE). SSE traditionally uses disposable syringes, which pose challenges in temperature control and waste generation.

Methods

This article experimentally simulates various scenarios relevant to pharmacy practice to evaluate the usability of the semi-solid extrusion approach using a first-of-its-kind reusable cartridge. The research assesses the stability of formulations under thermal stress conditions that simulate commercial settings, demonstrating the robust performance of this 3D drug printing method across multiple uses.

Results

This study introduces pharmaceutical-grade stainless-steel cartridges as a sustainable alternative to disposable syringes, enhancing temperature management and reducing waste in SSE 3D printing.

Conclusion

Our findings highlight the potential of reusable cartridges to improve efficiency and sustainability in pharmaceutical manufacturing, with implications for future formulation developments and stability studies. The presented 3D drugprinting approach offers a promising solution for environmentally responsible practices in pharmacy.

Purpose

Epalrestat is the most common Aldose reductase inhibitor (ARI) approved for blood glucose management in several countries and has also shown efficacy in preventing the onset of diabetic neuropathy (DN), and diabetic retinopathy. The present study aims to formulate and evaluate the effectiveness of Alginate beads of epalrestat in Streptozotocin-induced (STZ) diabetic rats in order to effectively manage the diabetes.

Method

Various formulations of Sodium cross-linked alginate beads containing epalrestat (F1 to F9) were prepared based on full factorial design by ionotropic gelation method. The formulations were characterized for particle size, % Drug entrapment efficiency (DEE), Fourier Transform Infra-Red Spectroscopy (FT-IR), Differential scanning calorimetry (DSC), X-ray Diffraction Study (X-RD), Scanning Electron Microscopy (SEM), and In-Vitro Release Studies. Optimized formulation (F6) [containing sodium alginate (2.5%w/v), epalrestat (2.5%w/v), and calcium chloride (2.5%w/v)] was subjected to in-Vivo efficacy testing in diabetic rats.

Result

Epalrestat-loaded beads were prepared (F1 to F9; Size = 3.21 μm; DEE = 97%) successfully using sodium alginate as polymer and calcium chloride solution as the crosslinking agent by modified ionotropic gelation method Optimized formulation showed a % DEE of 97% and highest drug release of 95% at the end of 10 hrs. Drug Release Kinetic of optimized formulation followed first-order kinetic. Further, the hypoglycemic effect was observed over a longer period 50% reduction after 2 hrs and continued till 4 hrs. In addition, normoglycemia was maintained till 12 hrs (20% reduction) in STZ-induced diabetic rats.

Conclusion

The formulation F6 was found to be superior compared to all the other formulations because the percentage drug entrapment efficiency was highest and there was no chemical interaction took place between the drug and polymer (Confirmed by DSC and XRD studies). In-vivo study showed prolonged hypoglycaemia till 12 hrs with a maximum reduction at 2 hrs Compared to plain drug suspension (20% reduction till 5 hrs).

Graphical Abstract