Controlled Drug Release Research Articles

Fabrication and evaluation of a biodegradable electrospun chip loaded with chlorhexidine for periodontal disease

Electrospinning technique is used for the manufacturing matrices of drug delivery systems. This study aimed at fabricating and evaluating an electrospun chip for prolonged retention and controlled drug release at the lesion site. A biodegradable electrospun chip loaded with chlorhexidine (BESC-CHX) was manufactured to treat periodontal diseases. Then, physicochemical properties and efficacy of BESC-CHXs were investigated. The CHX content of BESC was analyzed using high-performance liquid chromatography. The antimicrobial activity and anti-inflammation effects of BESC-CHX were assessed using a disc diffusion assay and a periodontal disease model. BESC-CHX, which is composed of 700 nm fibers, was observed by scanning electron microscopy. Many BESC-CHX batches maintained consistent CHX levels, with a drug entrapment efficiency of 83.3 %. The chip released CHX for seven days and was completely degraded in artificial saliva. BESC-CHX exhibited 99.99 % antimicrobial activity against 11 species of microorganisms. In a beagle periodontal disease model, BESC-CHX demonstrated improvements in periodontal probing depth and clinical attachment level, but these changes were not statistically significant. However, alveolar bone regeneration was observed in cementoenamel junction-alveolar bone crest measurements. The lowest inflammation scores were observed in this group. These findings suggest that BESC-CHXs may be beneficial for the treatment of periodontal disease.

Erlotinib and curcumin-loaded nanoparticles embedded in thermosensitive chitosan hydrogels for enhanced treatment of head and neck cancer

Head and neck squamous cell carcinoma (HNSCC) remain a major oncological challenge with significant morbidity and mortality rates. Erlotinib (Er) and Curcumin (Cm) are potential therapeutic agents for HNSCC, yet they are hindered by poor solubility and bioavailability. This study explored the optimization of poly(lactic-co-glycolic acid) nanoparticles co-loaded with Er and Cm (Er/Cm-NP), prepared via a D-optimal response surface design-guided nanoprecipitation process. The optimized formulation, optEr/Cm-NP, was then incorporated into chitosan/β-glycerophosphate hydrogels (optEr/Cm-NP-HG) to create an injectable intratumoral (IT) nanocomposite hydrogel (HG) delivery system. Physicochemical properties of the formulations, including gelation time, injectability, mechanical strength and drug release profiles were assessed alongside hemolytic activity. Compared to optEr/Cm-NP alone, the NP-loaded HG formulation exhibited a more pronounced modulation effect, enabling sustained and controlled drug release. The cytotoxicity of the developed formulations was evaluated using the FaDu HNSCC cancer cell line. Both optEr/Cm-NP and optEr/Cm-NP-HG21 displayed enhanced cytotoxicity compared to free drugs. Confocal laser microscopy and flow cytometry confirmed superior cellular uptake of Er and Cm when delivered via NPs or NP-loaded HG. Furthermore, a significant increase in apoptotic cell death upon treatment with optEr/Cm-NP was observed, highlighting its potential for HNSCC therapy. In vivo studies conducted on a xenograft HNSCC mouse model revealed the significant capacity of the intratumorally-injected optEr/Cm-NP-HG21 formulation to retard the tumor growth. Conclusively, the results presented herein report the successful development of a nanocomposite HG system incorporating NPs co-loaded with Er and Cm that could be efficiently utilized in the treatment of HNSCC.

Structure regulation of oxidized soybean cellulose nanocrystals/poly-acrylamide hydrogel and its application potential in wound dressing

The development of functional dressings based on natural polysaccharide-based hydrogels remains a great challenge, and the specific roles of gel composition and drug-controlled release mechanisms were unclear. In this study, oxidized soybean cellulose nanocrystals (CNCs)/poly-acrylamide (PAM) hydrogel was prepared. The proportion of CNCs, crosslinkers, and water in the system was regulated to fine-tune the rheological performances, texture properties, transparency, and micro-network structures of CNCs/PAM hydrogel, and further explored its application potential in the field of wound dressings. It was found that CNCs improved the rigidity and adhesion of hydrogels, crosslinkers improved the network density, and water promoted the softening and fluidity of hydrogels. The effective filling of CNCs in the composite hydrogel was verified by FTIR, XRD, and NMR. Furthermore, the pH responsiveness and drug-loading potential of the smart hydrogel were tested by swelling and drug-controlled release experiments, elucidating drug-release dynamic mechanisms during the wound healing process. The inhibition zones (>7 mm) of gram-positive/negative bacteria and cell viability (>100 %) assay showed satisfactory biocompatibility, as the hydrogel effectively accelerated wound healing in a wound model. These results elucidated the regulation mechanism of the structures of CNCs/PAM hydrogel and revealed the application potential of CNCs/PAM hydrogel in wound dressings.

Thymol-Loaded Polymeric Nanocapsules’ Repellent Activity on Nymphs of Rhipicephalus sanguineus Sensu Lato

Thymol-loaded polymeric nanocapsules were developed in this study to control volatilization and drug release for repellent application on Rhipicephalus sanguineus nymphs. Policaprolactone-loaded nanocapsules were prepared and characterized by diameter, PdI, zeta potential, pH, entrapment efficiency, and thymol content. Moreover, drug release, skin permeation profile, and repellent activity were evaluated. Nanocapsules showed a mean diameter of 195.7 ± 0.5 nm, a PdI of 0.20 ± 0.01, a zeta potential of −20.6 ± 0.3 mV, a pH of 4.7 ± 0.1, and an entrapment efficiency and a thymol content of 80.1 ± 0.1% and 97.9 ± 0.2%, respectively. The nanosystem progressively released 68.6 ± 2.3% of the thymol over 24 h, demonstrating that it can control drug release. Thymol-loaded nanocapsules showed less epidermis penetration upon skin application than pure thymol (control). Moreover, nanocapsules showed 60–70% repellency for 2 h against Rhipicephalus sanguineus nymphs. Thus, the nanocapsules proved to be a promising alternative for use as an arthropod repellent.

In situ growth of ZIF-8 on cellulose microspheres with high doxorubicin loading capacity and pH-sensitive for oral drug delivery

Metal-organic framework (MOF) nanoparticles are a class of porous nanomaterials with wide application prospects. Zeolitic imidazolate framework (ZIF) materials have high loading performance and pH-sensitive characteristics, which means they have great development prospects in the development of drug carrier systems. Herein, cellulose microspheres (CM) were used as a carrier for the nucleation and growth of ZIF-8 nanocrystals. CM@ZIF-8 was prepared in situ, which was more convenient, flexible, cost-effective, and highly safe. CM@ZIF-8, as a novel carrier, was used to monitor the release of the anticancer drug Doxorubicin (DOX) and prevent it from dissipating before reaching its goal. The designed DOX-loaded CM@ZIF-8 (CM@ZIF-8-DOX) system was characterized by FTIR, SEM, N2 sorption isotherm, XRD, and Cytotoxicity assay (cells survival rate 95.08 %). CM@ZIF-8-DOX exhibited controlled drug release behavior in simulated in-vitro tumor microenvironments (81.2 % drug release throughout 72h). CM@ZIF-8 simultaneously had a high loading capacity of DOX (Qe = 159.71 mg∙g−1), and the amount released under acidic conditions (pH 5.0) was greater (63.4 % after 15 h) than under neutral conditions (pH 7.4) due to the detachment of the coordination between metal ions and ligands (37.6 % after 15 h).

Microfabrication of controlled release osmotic drug delivery systems assembled from designed elements

ABSTRACT Background This study investigates combining 3D printing with traditional compression methods to develop a multicomponent, controlled-release drug delivery system (DDS). The system uses osmotic tablet layers and a semipermeable membrane to control drug release, similar to modular Lego® structures. Methods The DDS comprises two directly compressed tablet layers (push and pull) and a semipermeable membrane, all contained within a 3D-printed frame. The membrane is made from cellulose acetate and plasticizers like glycerol and propylene glycol. Various characterization techniques, including Positron Annihilation Lifetime Spectroscopy (PALS), were employed to evaluate microstructural properties, wettability, morphology, and drug dissolution. Results Glycerol improved the membrane’s wettability, as confirmed by PALS. The system achieved zero-order drug release, unaffected by stirring rates, due to the push and pull tablets within the 3D-printed frame. The release profile was stable, demonstrating effective drug delivery control. Conclusion The study successfully developed a prototype for a controlled-release osmotic DDS, achieving zero-order release kinetics for quinine hydrochloride after 2 h. This modular approach holds potential for personalized therapies in human and veterinary medicine, allowing customization at the point of care.

Enhancement of corrosion, biocompatibility and drug delivery properties of nitinol implants surface by Al-Zn-LDH nanohybrids

This study investigates the enhancement of drug delivery and corrosion resistance by incorporating dexamethasone sodium phosphate into aluminum-zinc layered double hydroxide (LDH) coated nickel-titanium alloys. The nickel-titanium samples were fabricated from titanium and nickel powders using spark plasma sintering (SPS) and cold press sintering (CPS), followed by electrophoretic deposition of LDH nanoparticles. This composite construction aims to utilize the biocompatibility and mechanical properties of nickel-titanium, combined with the controlled drug release and corrosion resistance properties of LDH coatings. Structural and microstructural characterizations were performed using X-ray diffraction and scanning electron microscopy. The results indicated that SPS samples exhibited superior microstructural homogeneity and corrosion resistance compared to CPS samples. Dexamethasone sodium phosphate was successfully intercalated into the LDH layers, as evidenced by an increase in layer spacing from 7.14 Å to 20.130 Å. The LDH-coated nickel-titanium with intercalated dexamethasone sodium phosphate demonstrated a 5 % lower drug release rate and significantly improved corrosion resistance compared to uncoated samples. Cell adhesion studies confirmed good biocompatibility between cells and the coated surface. This composite material shows promise for enhanced performance in biomedical applications, particularly in drug delivery and corrosion resistance.

Light-Responsive Smart Nanoliposomes: Harnessing the Azobenzene Moiety for Controlled Drug Release under Near-Infrared Irradiation.

The azobenzene moiety is an intriguing structure that deforms under UV and visible light, indicating a high potential for biomedical applications. However, its reaction to UV radiation is problematic because of its high energy and low tissue penetration. Unlike previous research on azobenzene structures in photoresponsive materials, this study presents a novel method for imparting photostimulation-responsive properties to liposomes by incorporating the azobenzene moiety and extending the light wavelength with up-conversion nanoparticles. First, the azobenzene structure was incorporated into a phospholipid molecule to create Azo-PSG, which could spontaneously form vesicle assemblies in aqueous solutions and isomerizes within 1 h of light exposure. Furthermore, orthogonal up-conversion nanoparticles with a core-shell structure were created by sequentially growing lanthanide rare earths in the shell layer, which efficiently converts near-infrared light into ultraviolet (400 nm) and blue-green (540 nm) light. Combining these core-shell structured up-conversion nanomaterials with Azo-PSG molecules resulted in the creation of a near-infrared light-responsive smart nanoliposome system. Under near-infrared light irradiation, UCNPs emit UV and blue-green light, causing conformational changes in Azo-PSG molecules that allow drug release within 6 h. The reversible structural shift of Azo-PSG in response to light stimulation holds enormous promise for improving drug release techniques. This novel technique also expands the usage of UV-responsive compounds beyond their constraints of low penetration and high biotoxicity, allowing for rapid medication release under NIR light.

Rapid Photoinduced Self-Healing, Controllable Drug Release, Skin Adhesion Ability, and Mechanical Stability of Hydrogels Incorporating Linker-Modified Gold Nanoparticles and Nanogels.

Appropriately modified thermoresponsive hydrogels, such as poly(N-isopropylacrylamide) hydrogels, bring an opportunity for a variety of biomedical applications. Incorporating compounds with different properties into poly(N-isopropylacrylamide) hydrogels offers opportunities to enhance their mechanical, self-healing ability, adhesiveness, thermal responsiveness, and drug release capabilities. In this study, we investigated the influence of Au-sulfur interactions on the properties of the poly(N-isopropylacrylamide) hydrogels after introducing N,N'-bis(acryloyl)cystine (a newly synthesized cross-linker), modified gold nanoparticles, and a p(NIPAm-BISS) nanogel into the hydrogel matrix. Our findings demonstrated that poly(N-isopropylacrylamide) hydrogels with these compounds exhibited higher mechanical strength (65% tensile stress and 25% elongation), faster thermal responsiveness, controllable self-healing [85% recovery after 2 min, using a NIR laser (800 nm, 0.75 W)], skin adhesiveness, and enhanced drug release (0.08 mg·mL-1, a 93% improvement). These results may contribute to advancements in the design of temperature-responsive hydrogels tailored for specific biomedical needs, such as targeted drug delivery with the use of a NIR laser and tissue engineering.

Controlled Drug Release Systems for Cerebrovascular Diseases

AbstractThis review offers a comprehensive exploration of optimized drug delivery systems tailored for controlled release and their crucial role in addressing cerebrovascular diseases. Through an in‐depth analysis, various controlled release methods, including nanoparticles, liposomes, hydrogels, and other emerging technologies are examined. Highlighting the importance of precise drug targeting, it is delved into the underlying mechanisms of these delivery systems and their potential to improve therapeutic outcomes while minimizing adverse effects. Additionally, the specific applications of these optimized drug delivery systems in treating cerebrovascular disorders such as ischemic stroke, cerebral aneurysms, and intracranial hemorrhage are discussed. By shedding light on the advancements in drug delivery techniques and their implications in cerebrovascular medicine, this review offers valuable insights into the future of therapeutic interventions in neurology.

Controlled drug release and antibacterial enhancement via NIR-activated CuS-modified TiO2 nanotubes arrays

Two primary obstacles impede the longevity of implants: bacterial infection and fixation loosening. This research introduces an innovative near-infrared (NIR) light-activated drug delivery system tailored to enhance the antimicrobial efficacy and bone integration of titanium-based implants. Titanium dioxide nanotube arrays (TNTs) were modified with epoxy for covalent bonding of therapeutic agents, and copper sulfide nanoparticles (CuS NPs) were added for regulated drug release. Alendronate sodium (ALN), an osteoporosis medication, was successfully bonded to the nanotubes. In vitro experiments showed that the release rate of ALN from TNTs-ALN reached 94 % within 36 h. In contrast, minimal release was observed in TNTs-ECH-ALN-CuS, which effectively addresses the prevalent issue of abrupt drug discharge typical in conventional delivery systems. In the context of NIR light exposure, the TNTs-ECH-ALN-CuS exhibited a notable ALN release efficacy of 48 %, demonstrating effective control over drug delivery. Additionally, the generation of ROS, coupled with temperature elevation under NIR exposure, endowed the modified TNTs with exceptional antibacterial efficacy, exceeding 99 % inhibition against E.coli and S.aureus. We observed a pronounced enhancement in the drug delivery mechanism, characterized by a reduction in the initial burst release and a sustained, controlled release, coupled with robust antibacterial action and notable biological performance.

Hydrogel Applications in the Diagnosis and Treatment of Glioblastoma.

Glioblastoma multiforme (GBM), a common malignant neurological tumor, has boundaries indistinguishable from those of normal tissue, making complete surgical removal ineffective. The blood-brain barrier (BBB) further impedes the efficacy of radiotherapy and chemotherapy, leading to suboptimal treatment outcomes and a heightened probability of recurrence. Hydrogels offer multiple advantages for GBM diagnosis and treatment, including overcoming the BBB for improved drug delivery, controlled drug release for long-term efficacy, and enhanced relaxation properties of magnetic resonance imaging (MRI) contrast agents. Hydrogels, with their excellent biocompatibility and customizability, can mimic the in vivo microenvironment, support tumor cell culture, enable drug screening, and facilitate the study of tumor invasion and metastasis. This paper reviews the classification of hydrogels and recent research for the diagnosis and treatment of GBM, including their applications as cell culture platforms and drugs including imaging contrast agents carriers. The mechanisms of drug release from hydrogels and methods to monitor the activity of hydrogel-loaded drugs are also discussed. This review is intended to facilitate a more comprehensive understanding of the current state of GBM research. It offers insights into the design of integrated hydrogel-based GBM diagnosis and treatment with the objective of achieving the desired therapeutic effect and improving the prognosis of GBM.

Development and optimization of guaifenesin sustained release mini-tablets for adult and geriatric patients.

Aim: The main aim of this study was to formulate and optimize sustained release mini-tablets of guaifenesin.Materials & methods: Guaifenesin granules were successfully prepared using different blend ratios of carnauba wax to drug by melt granulation method. The properties of granules were further modified by combining them with ethyl cellulose. The obtained granules were then mixed and compressed into mini-tablets using a tablet press machine. The resulting mini-tablets were characterized in terms of weight, thickness, hardness, drug content and in vitro drug release.Results: Mini-tablets with 1:6 carnauba wax to drug ratio showed superior physicochemical characteristics, releasing about 100.03% of guaifenesin over 8h. Ethyl cellulose offers a great potential to accurately control drug release from mini-tablets.Conclusion: The prepared mini-tablets seem to be a very promising alternative to guaifenesin conventional formulations and can be used in adults and elderly people.

Enzymatically Triggered Drug Release from Microgels Controlled by Glucose Concentration.

This study aims to design microgels for controlled drug release via enzymatically generated pH changes in the presence of glucose. Modern medicine is focused on developing smart delivery systems with controlled release capabilities. In response to this demand, we present the synthesis, characterization, and enzymatically triggered drug release behavior of microgels based on poly(acrylic acid) modified with glucose oxidase (GOx) (p(AA-BIS)-GOx). TEM images revealed that the sizes of air-dried p(AA-BIS)-GOx microgels were approximately 130 nm. DLS measurements showed glucose-triggered microgel size changes upon glucose addition, which depended on buffer concentration. Enzymatically triggered drug release experiments using doxorubicin-loaded microgels with immobilized GOx demonstrated that drug release is strongly dependent on glucose and buffer concentration. The highest differences in release triggered by 5 and 25 mM glucose were observed in HEPES buffer at concentrations of 3 and 9 mM. Under these conditions, 80 and 52% of DOX were released with 25 mM glucose, while 47 and 28% of DOX were released with 5 mM glucose. The interstitial glucose concentration in a tumor ranges from ∼15 to 50 mM. Normal fasting blood glucose levels are about 5.5 mM, and postprandial (2 h after a meal) glucose levels should be less than 7.8 mM. The obtained results highlight the microgel's potential for drug delivery using the enhanced permeability and retention (EPR) effect, where drug release is controlled by enzymatically generated pH changes in response to elevated glucose concentrations.

Enzyme-responsive microgel with controlled drug release, lubrication and adhesion capability for osteoarthritis attenuation

The treatment of osteoarthritis (OA) remains challenging due to the narrow therapeutic window and rapid clearance of therapeutic agents, even with intra-articular administration, resulting in a low treatment index. Recent advancements in local drug delivery systems have yet to overcome the issues of uncontrolled burst release and short retention time, leading to suboptimal OA treatment outcome. Herein, we developed a methacrylate-crosslinking hyaluronic acid (HA) microgel (abbreviated as CXB-HA-CBP) that covalently conjugates the anti-inflammatory drug celecoxib (CXB) via a metalloproteinase-2 (MMP-2)-responsive peptide linker (GGPLGLAGGC) and a collagen II binding peptide (WYRGRLC). The GGPLGLAGGC linker is specifically cleaved by the overexpressed MMP-2 enzyme within the OA joint, enabling the sustained and on-demand release of CXB entity. The synergistic action of CXB and HA effectively inhibited macrophage activation and reduced the production of pro-inflammatory cytokines, protecting chondrocytes from damage. Furthermore, the collagen II peptide introduced on the microgel surface enabled a cartilage-binding function to form an artificial lubrication microgel layer on the cartilage surface to reduce cartilage wear. The CXB-HA-CBP microgel showed an extended retention time of up to 18 days in the affected joint, leading to an effective OA treatment in rats. This sophistically designed microgel, characterized by the prolonged retention time, sustained drug delivery, and enhanced lubrication, presents a promising biomedicine for OA treatment. Statement of significanceA new methacrylate-crosslinking hyaluronic acid (HA) microgel, covalently conjugated with the celecoxib (CXB)-GGPLGLAGGC and the collagen II binding peptide (CBP, peptide sequence: WYRGRLC), was developed. The overexpressed MMP-2 in OA joint cleaved the GGPLGLAGGC linker to trigger the CXB moiety release. Besides, the CBP on the surface of microgels enabled a cartilage-attaching ability, resulting in a prolonged retention time and an improved lubrication property in joint. This advanced drug-loading microgel remarkably reduced macrophage activation and pro-inflammation cytokine production, while protecting the chondrocytes via a dual action of CXB and HA. This study demonstrated that the enzyme-responsive drug-loading microgel could serve as an platform to efficiently attenuate osteoarthritis.

3D printing novel enteric capsule shells for personalized drug delivery

Individualized drug delivery presents a viable strategy for enhancing medication efficacy and patient safety. It involves producing small batches of custom dosages tailored to each patient’s individual needs. However, current pharmaceutical manufacturing processes are not designed for personalized dosage forms. Additive manufacturing processes have great potential in the pharmaceutical industry due to the customizable nature of 3D printing technologies and the increasing demand for customized pharmaceutics and drug delivery systems. Conventional enteric capsules are prepared by dip coating to achieve gastro-resistant release, but the manufacturing process is erratic and unreliable. This study aimed to investigate the feasibility of manufacturing enteric capsules from enteric polymers using the hot melt extrusion (HME) and fused filament fabrication (FFF) process. HME was utilized to prepare filaments using enteric polymers, Hypromellose acetate succinate (HPMC-AS), and Eudragit-L 100–55, with plasticizers, sorbitol, and polyethylene glycol 4000 (PEG-4000), and a thermoplastic polymer, polyvinyl alcohol (PVA). A computer-aided design program was utilized to design size 0 capsules. The prepared capsule design and filaments were used to fabricate capsules using the FFF process. Powdered red dye was used to simulate the drug and its release from FFF fabricated capsules was evaluated in simulated gastric and intestinal fluids, pH 1.2 and 6.8, respectively. Various combinations of enteric polymer, plasticizer, and thermoplastic polymer were examined. Thermogravimetric analysis (TGA) showed that the temperatures used for processing polymer blends were well below their thermal degradation temperatures, and dye release profiles were generated using image analysis software. This study demonstrates that capsules made with HPMCAS, PEG-4000, and PVA via the FFF process are suitable for controlling drug release and that the release profile can be modified by making small changes to the formulation.

The Chitinous Skeleton of Ianthella basta Marine Demosponge as a Renewable Scaffold-Based Carrier of Antiseptics

The chitinous skeleton of the marine demosponge Ianthella basta exhibits a unique network-like 3D architecture, excellent capillary properties, and chemical inertness, making it highly suitable for interdisciplinary research, especially in biomedical applications. This study investigates the potential of renewable I. basta chitinous scaffolds for drug delivery and wound dressing. The scaffolds, characterized by a microtubular structure, were impregnated with selected commercially available antiseptics, including solutions with hydrophilic and hydrophobic properties. Evaluations against selected clinical strains of bacteria, as well as fungi, demonstrated significant zones of growth inhibition with antiseptics such as brilliant green, gentian violet, decamethoxine, and polyhexanide. Notably, the antibacterial properties of these antiseptic-treated chitin matrices persisted for over 72 h, effectively inhibiting microbial growth in fresh cultures. These findings highlight the considerable potential of I. basta chitin scaffolds as sustainable, innovative biomaterials for controlled drug release and wound dressing applications.

Advancements of metallic nanoparticles: A promising frontier in cancer treatment.

The incidence of cancer is increasing and evolving as a major source of mortality. Nanotechnology has garnered considerable scientific interest in recent decades and can offer a promising solution to the challenges encountered with traditional chemotherapy. Nanoparticle utilization holds promise in combating cancer and other diseases, offering exciting prospects for drug delivery systems and medicinal applications. Metallic nanoparticles exhibit remarkable physical and chemical properties, such as their minute size, chemical composition, structure, and extensive surface area, rendering them versatile and cost-effective. Research has demonstrated their significant and beneficial impact on cancer treatment, characterized by enhanced targeting abilities, gene activity suppression, and improved drug delivery efficiency. By incorporating targeting ligands, functionalized metal nanoparticles ensure precise energy deposition within tumors, thereby augmenting treatment accuracy. Moreover, beyond their therapeutic efficacy, metal nanoparticles serve as valuable tools for cancer cell visualization, contributing to diagnostic techniques. Utilizing metal nanoparticles in therapeutic systems allows for simultaneous cancer diagnosis and treatment, while also facilitating controlled drug release, thus revolutionizing cancer care. This narrative review investigates the advancements of metal nanoparticles in cancer treatment, types and mechanisms in targeting cancer cells, application in clinical scenarios, and potential toxicity in medicine.

Preparation, Swelling, and Drug Release Studies of Chitosan-based Hydrogels for Controlled Delivery of Buspirone Hydrochloride.

Buspirone is used for the management of depression and anxiety disorders. Due to its short half-life and low bioavailability, it requires multiple daily doses and is associated with some side effects. This study aimed to develop chitosan-based hydrogels as drug-controlled release carriers. The objective of this study is to prepare chitosan-based hydrogels as controlled release carriers in order to overcome the side effects of buspirone HCl and improve patients' compliance and their life quality. Polymer chitosan was polymerized with two monomers, acrylic acid and itaconic acid, to synthesize pH-sensitive hydrogel. The Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) analysis were performed to confirm the structure formation and thermal stability. Water penetration capability and loading of the drug were performed by porosity and drug loading studies. The swelling and dissolution tests were performed to analyze the pH-sensitive nature of the developed hydrogels. FTIR, TGA, and DSC demonstrated that the chitosan-based hydrogels were successfully prepared. An increase in water penetration and drug loading into the hydrogel network was seen with the high incorporation of chitosan, acrylic acid, and itaconic acid. The swelling and dissolution studies revealed that prepared hydrogel offered the greatest swelling and drug release at a high pH of 7.4. The swelling and drug release from the hydrogel were affected by the concentrations of the incorporated contents. A controlled release of the drug was achieved by using chitosan-based hydrogel as a delivery carrier compared to commercial tablets of buspirone. The results showed that the developed chitosan-based hydrogel can be considered one of the most suitable drug carrier systems for the controlled delivery of buspirone.

Evaluation of polymer combinations in vaginal mucoadhesive tablets for the extended release of acyclovir

Genital herpes, caused by herpes simplex virus type 2 (HSV-2), affects nearly 500 million people, mostly women. Since the main route of transmission is sexual contact, the development of an acyclovir extended-release vaginal microbicide would be a suitable tool for the prevention of virus transmission. In this work, we evaluated the potential of three polymers with different characteristics (chitosan, xanthan gum and ethyl cellulose) for obtaining acyclovir extended-release vaginal tablets. By combining the polymers, certain useful synergies were observed to modify their mucoadhesive capacity and control drug release. In the swelling studies, it observed that a polyelectrolyte complex with more moderate swelling and sustained gelation was formed between chitosan and xanthan gum exclusively in acidic medium (simulated vaginal fluid). This complex allowed prolonging the mucoadhesion of the tablets in ex vivo studies performed with vaginal mucosa, which would translate into better retention in the vagina after administration. In addition, the combination of chitosan and xanthan gum allowed obtaining a controlled release of acyclovir for 5 days, regardless of the pH of the medium, which would guarantee that drug release continues even in the presence of seminal fluid.