Sustained Release Effect Research Articles

Bioadhesive Microcarriers Encapsulated with IL-27 High Expressive MSC Extracellular Vesicles for Inflammatory Bowel Disease Treatment.

Mesenchymal stem cell (MSC) therapy is a promising candidate for inflammatory bowel disease (IBD) treatment, while overcoming the limitations of naive seeding cells function and realizing efficient intestinal targeting remains a challenge. Here, a bioadhesive microparticle carrying interleukin-27 (IL-27) MSC-derived extracellular vesicles (MSCIL-27 EVs) is developed to treat IBD. The MSCIL-27 EVs prepared through lentivirus-mediated gene transfection technology show ideal anti-inflammatory and damage repair function. By encapsulating MSCIL-27 EVs into dopamine methacrylamide-modified hydrogel, a bioadhesive EVs microcarrier via microfluidic technology is fabricated. The resultant microcarriers exhibit ideal MSCIL-27 EVs sustained release effect and effective wet adhesion property. Furthermore, the therapeutic potential of MSCIL-27 EVs-loaded microcarriers in treating IBD is demonstrated. Through giving IBD rats a rectal administration, it is found that the microcarriers can firmly anchor to the surface of colon, reduce the inflammatory response, and repair the damaged barrier. Therefore, the bioadhesive MSCIL-27 EVs-loaded microcarriers provide a promising strategy for the biomedical application of MSC-derived EVs, and broaden the clinical potential of MSC therapy.

Improved sustained-release properties of ginger essential oil in a Pickering emulsion system incorporated in sodium alginate film and delayed postharvest senescence of mango fruits

The insufficient water vapor barrier and mechanical capacity of sodium alginate (SA) film limited its application in fruit preservation. Herein, cellulose nanocrystals (CNCs) were used to stabilize Pickering emulsion. Then, we prepared SA composite films. Ginger essential oil (GEO) was loaded as antimicrobials and antioxidants. Finally, the application on mangos were investigated. Compared to coarse emulsion, Pickering emulsion and its film-formation-solution showed more stable system and larger droplet size. The emulsion significantly changed the properties of SA film. Specifically, CNCs improved the thermal, tensile, and barrier properties of the film and GEO enhanced the ultraviolet-visible light barrier capacity. Additionally, the SA/CNC film possessed a homogeneous micromorphology which had a sustained-release effect on GEO, thus maintaining high postharvest quality and long-term bioavailability for mangos. In conclusion, the film prepared via Pickering emulsion showed satisfactory properties which had great potential in fruit preservation.

Manganese-doped albumin-gelatin composite nanogel loaded with berberine applied to the treatment of gouty arthritis in rats via a SPARC-dependent mechanism

In this study, manganese-doped albumin-gelatin composite nanogels (MAGN) were prepared and used to load berberine (Ber) for the treatment of gouty arthritis (GA). The nanodrug delivery system (Ber-MAGN) can target inflammatory joints due to the intrinsic high affinity of albumin for SPARC, which is overexpressed at the inflammatory site of GA. Characterization of the pharmaceutical properties in vitro showed that Ber-MAGN had good dispersion, and the particle size was 121 ± 10.7 nm. The sustained release effect significantly improved the bioavailability of berberine. In vitro and in vivo experimental results showed that Ber-MAGN has better therapeutic effects in relieving oxidative stress and suppressing inflammation. Therefore, Ber-MAGN, as a potential pharmaceutical preparation for GA, provides a new reference for the clinical treatment plan of GA.

Formulation Development and Evaluation of Wax Incorporated Floating Beads of Dapagliflozin

Introduction: The current work's objectives are to build numerous floating drug delivery systems utilising various wax concentrations to prolong the release of dapagliflozin and to study the influence of sodium alginate on the system's buoyancy. Dapagliflozin is used as a anti diabetic drug which is used in treatment of type-2 diabetes.The goal of the study is to create sodium-based emulsion gel beads with wax incorporated utilising a modified emulsion-gelation process. Method: Emulsion gelation method used for preparation of floating beads. The Model drug was mixed with olive oil-containing sodium alginate wax before being hot-melted, homogenised, and then extruded into a calcium chloride solution. The manufactured Wax-incorporated Emulsion Gel Beads were analysed for Micromeritics investigations, entrapment efficacy, in-vitro buoyancy rate, and dissolution rate. Result: Several preformulation experiments, including bulk density, tapped density, and Carr's index, were within acceptable ranges, and highest drug release after 12 hours is 96.63% particularly for batch F2. Wax was added to the formulation to greatly extend the drug release; however, it was not enough to maintain the release of a highly water-soluble medication. Conclusion: It is possible to conclude that the usage of hydrophobic carriers such as waxes can be used to provide the desired sustained release effect. Oils and other low-density components were utilised to help the formulation's flotation. The study concluded that floating wax microspheres may use as medication carrier to prolong drug release.

A curcumin oral delivery system based on sodium caseinate and carboxymethylpachymaran nanocomposites

The food industry has paid lots of attentions to curcumin because of its potential bioactive qualities. However, its use is severely constrained by its low bioavailability, stability and water solubility. Herein, we created sodium caseinate and carboxymethylpachymaran (CMP) nanoparticles (SMCNPs) that were loaded with curcumin. The composite nanoparticles were spherical, as characterized by SEM and TEM, the fluorescence spectroscopy, FTIR and XRD research revealed that hydrogen bonding, hydrophobic interaction and electrostatic interaction were the main drivers behind the creation of the nanoparticles. The SMCNPs exhibited lower particle size, greater dispersion and higher encapsulation rate when the mass ratio of sodium caseinate to CMP was 3:5 (particle size of 166.8 nm, PDI of 0.15, and encapsulation efficiency of 88.07 %). The composite nanoparticles had good antioxidant activity, physical stability and sustained release effect on intestinal tract during the in vitro simulation experiments, successfully preventing the early release of curcumin into gastric fluid. Finally, cytotoxicity studies told that the prepared composite nanoparticles have good biocompatibility and can inhibit the growth of tumor cells (HT-29). In conclusion, using CMP and sodium caseinate as carriers in this study may open up a fresh, environmentally friendly, and long-lasting way to construct a bioactive material delivery system.

A bio-inspired nanoparticle coating for vascular healing and immunomodulatory by cGMP-PKG and NF-kappa B signaling pathways

Drug-eluting stents (DESs) implantation is an effective method to tackle in-stent restenosis (ISR), which has been considered as an efficient treatment for coronary atherosclerosis. Although fruitful results have been achieved in treating coronary artery diseases (CAD), concern has arisen regarding the long-term safety and efficacy of DESs, primarily due to adverse events such as delayed re-endothelialization, persistent inflammatory response, and late stent thrombosis (LST). Taking inspiration from the immunomodulatory functions of camouflage strategies, this study designed a bio-inspired nanoparticle-coated stent. Briefly, the platelet membrane-coated poly (lactic-co-glycolic acid)/Rapamycin nanoparticles (PNP) were sprayed onto stents, forming a homogenous nanoparticle coating. The bilayer of poly (lactic-co-glycolic acid) (PLGA) and platelet membrane works synergistically to promote the sustained-release effect of rapamycin. In vitro studies revealed that the PNP-coated surfaces promoted the competitive adhesion of endothelia cells while inhibiting smooth muscle cells. Subsequent in vivo studies demonstrated that these surfaces expedite re-endothelialization and elicit immunomodulatory effects by regulating the cGMP-PKG and NF-kappa B signaling pathways, influencing the biosynthesis cofactors and immune system signaling. The study successfully deviced a novel and biomimetic drug-eluting stent system, unraveling its detailed functions and molecular mechanism of action for enhanced vascular healing.

A Novel PTH-Related Peptide Combined With 3D Printed Macroporous Titanium Alloy Scaffold Enhances Osteoporotic Osseointegration.

Previous parathyroid hormone (PTH)-related peptides (PTHrPs) cannot be used to prevent implant loosening in osteoporosis patients due to the catabolic effect of local sustained release. A novel PTHrP (PTHrP-2) that can be used locally to promote osseointegration of macroporous titanium alloy scaffold (mTAS) and counteract implant slippage in osteoporosis patients is designed. In vitro, PTHrP-2 enhances the proliferation, adhesion, and osteogenic differentiation of bone marrow-derived mesenchymal stem cells (BMSCs) within the mTAS. Further, it promotes proliferation, migration, angiogenesis-related protein expression, and angiogenesis in human umbilical vein endothelial cells (HUVECs). Compared to PTH(1-34), PTHrP-2 can partially weaken the osteoclast differentiation of RAW 264.7 cells. Even in an oxidative stress microenvironment, PTHrP-2 safeguards the proliferation and migration of BMSCs and HUVECs, reduces reactive oxygen species generation and mitochondrial damage, and partially preserves the angiogenesis of HUVECs. In the Sprague-Dawley (SD) rat osteoporosis model, the therapeutic benefits of PTHrP-2-releasing mTAS (mTASP2 ) and ordinary mTAS implanted for 12 weeks via micro-CT, sequential fluorescent labeling, and histology are compared. The results demonstrate that mTASP2 exhibits high bone growth rate, without osteophyte formation. Consequently, PTHrP-2 exhibits unique local synthesis properties and holds the potential for assisting the osseointegration of alloy implants in osteoporosis patients.

Design and evaluation of gastro-swelling/gastro-floating sustained-release tablets of brivaracetam for epilepsy therapy

To prolong the absorption of the drug and achieve the effect of gastric retention, new brivaracetam tablets together with the characteristics of rapid swelling and sustained floating have been developed here. The tablets were optimized and prepared by direct compression techniques using Kollidon® SR and cross-linked polyvinylpyrrolidone (PVPP) XL as the matrix and disintegrant respectively, and carbomer 71G NF and polyethylene oxide (PEO) N60K as the gel materials to achieve sustained release effect. The characteristics of static expansion, floating time, drug release and dynamic swelling performance in vitro of the tablets were evaluated. The optimized formulations (F5 and F10) exhibited satisfactory swelling and floating properties, mechanical strength, and in vitro sustained-release characteristic with diffusion and matrix erosion mechanisms. X-ray images of beagle dogs showed that the tablet F5 could be retained in the stomach for more than 6 h. Furthermore, the pharmacokinetic studies in volunteers exhibited that the bioavailability of F5 and F10 was 95.70% (90% CI, 83.80%-109.28%) and 103.39% (90% CI, 87.61%-122.01%), respectively, relative to commercial tablets, with Tmax prolonged, demonstrating an excellent sustained-release effect. Therefore, the present system can reduce dosing frequency and improve patient compliance, which is expected to be a promising treatment option for epilepsy patients.

Gelatin-Functionalized Carbon Nanotubes Loaded with Cisplatin for Anti-Cancer Therapy.

Cisplatin (Cp), a chemotherapeutic agent, interacts with purines on tumor DNA, causing tumor cell apoptosis. However, cisplatin has the characteristics of non-specific distribution and lack of selectivity, resulting in systemic toxicity. Moreover, it cannot maintain the drug's high concentration in the tumor-weak acid environment. These flaws of cisplatin restrict its use in clinical applications. Therefore, a pH-responsive carbon nanotube-modified nano-drug delivery system (CNTs/Gel/Cp) was constructed in this study using gelatin (Gel)-modified carbon nanotubes (CNTs/Gel) loaded with cisplatin to release drugs precisely and slowly, preventing premature inactivation and maintaining an effective concentration. When MCp:MCNTs/Gel = 1:1, the drug reaches the highest loading rate and entrapment efficiency. To achieve the sustained-release effect, CNTs/Gel/Cp can release the medicine steadily for a long time in a pH environment of 6.0. Additionally, CNTs/Gel/Cp display antitumor properties comparable to cisplatin in a manner that varies with the dosage administered. These findings indicate that CNTs/Gel/Cp have an effective, sustained release of cisplatin and a good antitumor effect, providing a theoretical and experimental basis for the clinical application of modified carbon nanotubes (CNTs) as a new drug delivery system.

Development and characterization of AgHNTs@SPU film loaded with letrozole as drug delivery system and its anticancer activity

Polyurethane is an excellent implant biomaterial due to its elasticity, flexibility, resistance to abrasions and chemicals, and highly hydrophobic nature. The risk of hydrophobic nature is a significant drawback for an ideal drug delivery system. To enhance the hydrophilicity and compatibility of polyurethane via surface modification, such as (1) Introducing salicylic acid into the polymer backbone can create voids for the release of drugs from the matrix. (2) Doping silver onto HNTs by a simple one-pot precipitation method can enable silver to rupture the nucleus of cancer cells and induce ROS formation. The polyurethane and its mixed matrix were cast into the film to improve the initial effect of the drug, duration, and dosing than other conventional methods. The benefits of surface modification and thin film technology resulted in degradability, cytocompatibility, and excellent anticancer activity. The in vitro release studies depict that the letrozole-loaded film has a sustained release effect for a longer period based on the swelling ratio. The MTT assay showed that the [email protected] film could cause THP-1 cell death due to silver, polyols of PU, and HNTs. Salicylic acid played a vital role in increasing the antibacterial activity of the film. Furthermore, the increased oxidative stress was seen in [email protected]/Let film due to the biomaterial's active presence. Thus, [email protected]/Let a film is a potential approach for producing an implantable anticancer drug delivery system for the future with higher tumor cell death and prolonged drug release.

Nanocomposite hydrogels: an optimistic insight towards the treatments of ocular disorders.

The distinct anatomy and physiology of the eye represent it as a specialized organ. The noumenal physiological barriers, whose prominent role is to prevent the entrance of extracellular substances, reduce the bioavailability of medicines taken locally. Nanocarriers offer many advantages, such as site-specific drug delivery, reduced dose-related side effects, more drug loading capacity, etc. Nanoparticles, nano micelles, Nanostructured Lipid Carriers (NLCs), Solid Lipid Nanoparticles (SLNs), liposomes, polymeric nanoparticles, microspheres, microemulsions, etc., have all undergone significant analysis to overcome numerous static and dynamic obstacles. Among the several methods of delivering drugs, one of the most captivating and demanding is ocular drug delivery (ODD). The intent of developing formulations for an extended period can be partially achieved via thermoresponsive hydrogels. It is feasible to store fluids inside a cross-linked gel system for efficient long-term administration owing to hydrogels, which are hydrophilic polymeric networks with excellent three-dimensional structures and water or biological fluid absorption capacities. Hydrogels can be incorporated into nanocarriers to achieve site-specific action and prolonged release. Related patents and research reports with various platforms like Science Direct, Springer, PubMed, Google Scholar, Shodhganga, and Patseer were used to gather the data, and a search methodology was availed. The paper thoroughly summarizes the strategies for incorporating drugs with hydrogel into a nanocarrier to provide sustained release and prolonged therapeutic effects. According to the comprehensive review of literature and patents like (US2015374633A1), (US10980882B2), and (WO2011018800A2), nanocarrier-loaded thermoresponsive hydrogels show promising results. Due to their propensity to alter state in reaction to temperature changes, thermoresponsive hydrogels can improve medication bioavailability. Intervening nanocarriers loaded hydrogels directly on the targeted site displays local intervention and site-specificity. Thus, the use of nanocarriers in ocular drug delivery is encouraging.

PREPARATION OF DRUG-LOADED CHITOSAN/HYDROXYAPATITE COMPOSITE MATERIAL AND ITS NUMERICAL SIMULATION IN NASAL DEFECT REPAIR

With the continuous innovation and development of materials science and tissue engineering technology, biomaterials are gradually being used to replace autologous bone and allogeneic bone grafts in clinical practice for the treatment and repair of bone defects. In this paper, L-arginine-modified chitosan/hydroxyapatite composites were prepared by solution blending of L-arginine-modified chitosan and hydroxyapatite. A hormone drug prednisone acetate was loaded into the composites by supercritical impregnation technique. The results of in vitro release showed that under the loading condition of 12 MPa and 318 K, the cumulative release amount of the drug was 74.6% in 72 h, which had an excellent sustained release effect. In addition, a numerical model of the nasal bone was developed and numerical calculations were performed to analyze and compare the stresses of the healthy nasal bone and the nasal bone repaired with CA/HA composite when subjected to a force of 100 N, in different directions. The total deformation difference at the material was 0.002-0.004 mm/mm, and the stress difference was 0.004–1.373 MPa for the nasal bone in both states, with the sagittal plane under 0–90 degrees of force. The above results indicate that the CA/HA composite has good biological and mechanical properties and can be used to repair nasal bone defects. This material and numerical calculation method can also be applied to other related bone tissue engineering and biomedical materials, which have broad application prospects.

Preparation and properties of gelatin-tannic acid histidine metal complex microspheres

Tannin histidine metal complex is a type of synthetic analogues of superoxide dismutase. To make the most of its SOD-like activity and expand its value in medical field, the gelatin-tannic acid histidine metal complex microspheres were prepared by emulsion cross-linking method. The optimum conditions for preparation of microspheres are found based on encapsulation ratio and the encapsulation efficiency range of four types of complex microspheres is 89.90–93.57 % under these conditions. The microspheres were characterized by IF spectrum, SEM and particle size analysis. The results showed that the average particle size of the four kinds of microspheres ranged from 5.5 to 14.7 μm. Certain properties of microspheres were investigated and results prove that they have a high antioxidant property and a good sustained release effect, meanwhile, the optimal storage temperature and stable kinetic model are obtained. The study provides a way for the application of superoxide dismutase mimics in the sustained release.

A sustained-release phospholipid-based phase separation gel loaded with berberine for treating rheumatoid arthritis.

Berberine (BBR) has a long history of use in the treatment of Rheumatoid arthritis (RA) and is considered one of the most promising natural product for the treatment of RA. However, oral administration of berberine has low bioavailability and requires frequent administration, resulting in poor patient compliance. In this study, we developed a BBR-loaded phospholipid-based phase separation gel (BBR-PPSG) to achieve sustained drug release and long-term therapeutic effect. The stability of BBR-PPSG was verified and it was found that it can be stored for a long time. The pharmacokinetic study on rats and rabbits showed that BBR-PPSG not only achieved 1-month of sustained release, but also significantly increased the area under the curve (AUC) by nearly 9-fold and prolonged the half-life (t1/2) by 10-fold. By constructing rat and rabbit models of RA, we also proved that BBR-PPSG administration once a month effectively alleviated joint swelling, and significantly reduce TNF-α levels in AIA rats and OIA rabbits. Histopathological analysis of rabbit joint sections revealed that after intra-articular injection of BBR-PPSG, the synovial cell layer remained intact, while in the model group, the synovial cells were significantly reduced and exhibited necrosis. MicroCT data analysis showed that the values of Tb.N and Tb. Sp in the BBR-PPSG group were significantly better than those in the model group (p < 0.05). This study addressed the limitations of frequent administration of BBR by developing a phospholipid-based phase separation gel system for berberine delivery, achieving long-term sustained release. The BBR-PPSG demonstrated good biocompatibility, simple preparation and excellent stability, thus holding potential as a novel pharmaceutical formulation for RA treatment.

Construction of multi-program responsive vitamin E succinate-chitosan-histidine nanocarrier and its response strategy in tumor therapy

Multifunctional drug delivery carriers have emerged as a promising cancer drug delivery strategy. Here, we developed a vitamin E succinate-chitosan-histidine (VCH) multi-program responsive drug carrier. The structure was characterized by FT-IR and 1H NMR spectrum, and the DLS and SEM results showed typical nanostructures. The drug loading content was 21.0 % and the corresponding encapsulation efficiency was 66.6 %. The UV–vis and fluorescence spectra demonstrated the existence of the π-π stacking interaction between DOX and VCH. Drug release experiments implied good pH sensitivity and sustained-release effect. The DOX/VCH nanoparticles could be efficiently taken up by HepG2 cancer cells and the tumor inhibition rate was up to 56.27 %. The DOX/VCH reduced the tumor volume and weight efficiently with a TIR of 45.81 %. The histological analysis results showed that DOX/VCH could effectively inhibit tumor growth and proliferation, and there was no damage to normal organs. VCH nanocarriers could combine the advantages of VES, histidine and chitosan to achieve pH sensitivity and P-gp inhibition, and effectively improve the drug solubility, targeting and lysosomal escape. Through the program response of different micro-environment, the newly developed polymeric micelles could successfully be utilized as a multi-program responsive nanocarrier system for the treatment of cancers.

Construction and properties of venlafaxine hydrochloride sustained release system based on hollow mesoporous silica microspheres

The aim of this work is to develop a venlafaxine hydrochloride sustained release system based on hollow mesoporous silica microspheres (HMSMs). HMSMs were innovatively prepared with tetraethyl silicate (TEOS) as the precursor and volatile n-heptane as a soft template. The obtained HMSMs show a well-defined hollow structure with an average size of 967 nm and pore volume of 0.85 cm3/g, implying it is a potential drug carrier. Subsequently, venlafaxine hydrochloride (VF) was absorbed in the HMSMs with a content of 37.67% or so. The sustained release effect is further measured by the dissolution instrument at 37 °C and 50 rpm in ultrapure water. The results showed that the HMSMs/VF system shows good sustained release properties compared with sustained release tablets with hydroxypropyl methylcellulose as the main component. This HMSMs sustained release system appears to be a promising candidate for a sustained drug release.

Study on Preparation and Mechanism of Concrete Slump Retaining Agent

Using acrylic acid and polyether polymer as the main raw materials, with hydroxyethyl acrylate monomer free radical copolymerization of polycarboxylic acid slump inhibitor, has the effect of reducing the slump loss of concrete. The slow release rate of concrete slump retaining agent synthesized with different ester ratios was studied, and the effects of different ester ratios, different ester ether ratios, and different ambient temperatures on the dispersion, dispersion retention, and hydrolysis rate of polycarboxylic acid slump retaining agent were systematically studied. The knowledge basis for the development of the slump-retaining agent with different sustained release effects. In engineering applications, the working performance of concrete can be controlled more effectively according to the length of the slow release time.

High drug loading hydrophobic cross-linked dextran microspheres as novel drug delivery systems for the treatment of osteoarthritis

Drug delivery via intra-articular (IA) injection has proved to be effective in osteoarthritis (OA) therapy, limited by the drug efficiency and short retention time of the drug delivery systems (DDSs). Herein, a series of modified cross-linked dextran (Sephadex, S0) was fabricated by respectively grafting with linear alkyl chains, branched alkyl chains or aromatic chain, and acted as DDSs after ibuprofen (Ibu) loading for OA therapy. This DDSs expressed sustained drug release, excellent anti-inflammatory and chondroprotective effects both in IL-1β induced chondrocytes and OA joints. Specifically, the introduction of a longer hydrophobic chain, particularly an aromatic chain, distinctly improved the hydrophobicity of S0, increased Ibu loading efficiency, and further led to significantly improving OA therapeutic effects. Therefore, hydrophobic microspheres with greatly improved drug loading ratio and prolonged degradation rates show great potential to act as DDSs for OA therapy.

Pharmacokinetic Evaluation of Telmisartan and Cilnidipine Bilayer Tablet in A Rabbit Model

Hypertension is a chronic medical condition affecting a significant proportion of the global population. It is a major risk factor for cardiovascular diseases, stroke, and kidney failure. Telmisartan and cilnidipine combination are commonly used in managing hypertension due to their complementary mechanism of action. Therefore, a bilayer tablet design that enhances the pharmacokinetic profile of cilnidipine as a sustained-release drug while telmisartan act as an immediate-release drug may provide a better therapeutic option for hypertension management. We aim to evaluate the pharmacokinetic parameters of the bilayer tablet of Telmisartan and Cilnidipine. Our objective is to observe the bioavailability of the bilayer tablet in rabbit plasma. The formulation aims to achieve an immediate release effect for Telmisartan and a sustained release effect for Cilnidipine. The solubility and bioavailability of Telmisartan were enhanced by complexation with beta-cyclodextrin. To achieve our aim, we observe the drug concentration in rabbit plasma. Telmisartan is an angiotensin receptor blocker, while Cilnidipine is a calcium channel blocker. The pharmacokinetics of the drugs were evaluated in New Zealand rabbits following oral administration. Systemic drug bioavailability was assessed, and an HPLC method was developed to estimate Telmisartan and Cilnidipine's plasma concentration simultaneously. A Gemini C-18 column (250 mm X 4.6 mm X 5 microns) Phenomenex was used for peak separation. The mobile phase consisted of acetonitrile with phosphate buffer pH 3.5 v/v, with a flow rate of 1.5 ml per minute. The calibration curve analysis indicated a correlation coefficient of 0.9996 and 0.9997 for Telmisartan and Cilnidipine, respectively. The pharmacokinetics of the optimized batch, including Cmax, Tmax, and AUC values, were compared to those of the pure drug. Drug concentration was detected using a DAD detector with an excitation wavelength of 241nm. No interaction was observed between the drugs and excipients. The in-vivo study of the formulation showed higher bioavailability, indicating that the developed bilayer tablet formulation could be an effective means of delivering Telmisartan and Cilnidipine.

Development and evaluation of finasteride niosomes targeting to hair follicles for the management of androgenic alopecia

Finasteride, a selective Type II 5α-reductase inhibitor, has been approved as an oral drug for the treatment and prevention of androgenetic alopecia (AGA). The daily administration of finasteride by oral route may lead to various undesirable systemic side effects. In the present study, finasteride niosomes (FIN-NIS) as a dermal topical delivery system were developed evaluated in vitro/in vivo in an attempt to overcome the limitations of the oral administration of finasteride, enhance the retention of finasteride into hair follicles, and cause fewer adverse effects. FIN-NIS were prepared by ethanol injection method and characterized for particle size, entrapment efficiency (EE), in vitro release and in vitro skin retention. Testosterone-induced AGA mice model was used to evaluate the therapeutic effect of FIN-NIS. The results show that the particle size of FIN-NIS was about 260 nm with a good loading capacity, and the EE was greater than 90%. FIN-NIS had the sustained-release effect to some extent. Compared with the hydroethanolic solution of finasteride (FIN-hydroethanol) and finasteride suspension (FIN-suspension), FIN-NIS showed higher drug concentration in the excised rat skin, especially in the hair follicle area. The drug accumulation of FIN-NIS in the hair follicles was 20 times higher than that of FIN-hydroalcohol. In addition, FIN-NIS was more effective to promote hair regeneration in AGA mice than FIN-suspension, and the effectiveness of FIN-NIS even exceeded that of minoxidil. In conclusion, FIN-NIS could become a promising dermal topical delivery system for enhancing the performance of finasteride for the management of AGA and avoiding the possible risk of systemic side effects associated with oral administration.