{"title":"Overcoming Skin Barrier with Transfersomes: Opportunities, Challenges, and Applications.","authors":"Bhupendra Dixena, Rashmi Madhariya, Anupama Panday, Alpana Ram, Akhlesh K Jain","doi":"10.2174/0115672018272012231213100535","DOIUrl":"https://doi.org/10.2174/0115672018272012231213100535","url":null,"abstract":"<p><strong>Background: </strong>Transdermal drug delivery systems (TDDS) offer several advantages over traditional methods like injections and oral administration, including preventing first-pass metabolism, providing consistent and sustained activity, reducing side effects, enabling the use of short halflife drugs, improving physiological response, and enhancing patient convenience. However, the permeability of skin poses a challenge for TDDS, as it is impermeable to large molecules and hydrophilic drugs but permeable to small molecules and lipophilic medications. To overcome this barrier, researchers have investigated vesicular systems, such as transfersomes, liposomes, niosomes, and ethosomes. Among these vesicular systems, transfersomes are particularly promising for non-invasive drug administration due to their deformability and flexible membrane. They have been extensively studied for delivering anticancer drugs, insulin, corticosteroids, herbal medicines, and NSAIDs through the skin. Transfersomes have demonstrated efficacy in treating skin cancer, improving insulin delivery, enhancing site-specific corticosteroid delivery, and increasing the permeation and therapeutic effects of herbal medicines. They have also been effective in delivering pain relief with minimal side effects using NSAIDs and opioids. Transfersomes have been used for transdermal immunization and targeted drug delivery, offering site-specific release and minimizing adverse effects. Overall, transfersomes are a promising approach for transdermal drug delivery in various therapeutic applications.</p><p><strong>Objectives: </strong>The aim of the present review is to discuss the various advantages and limitations of transfersomes and their mechanism to penetration across the skin, as well as their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.</p><p><strong>Methods: </strong>Data we searched from PubMed, Google Scholar, and ScienceDirect.</p><p><strong>Results: </strong>In this review, we have explored the various methods of preparation of transferosomes and their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.</p><p><strong>Conclusion: </strong>In comparison to other vesicular systems, transfersomes are more flexible, have greater skin penetration capability, can transport systemic medicines, and are more stable. Transfersomes are capable of delivering both hydrophilic and hydrophobic drugs, making them suitable for transdermal drug delivery. The developed transfersomal gel could be used to improve medicine delivery through the skin.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139099457","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"A Comprehensive Review on Imperative Role of Ionic Liquids in Pharmaceutical Sciences.","authors":"Prerna Uniyal, Shibam Das, Surbhi Panwar, Neelima Kukreti, Pankaj Nainwal, Rohit Bhatia","doi":"10.2174/0115672018255191230921035859","DOIUrl":"10.2174/0115672018255191230921035859","url":null,"abstract":"<p><p>Ionic liquids (ILs) are poorly-coordinated ionic salts that can exist as a liquid at room temperatures (or <100 °C). ILs are also referred to as \"designer solvents\" because so many of them have been created to solve particular synthetic issues. ILs are regarded as \"green solvents\" because they have several distinctive qualities, including better ionic conduction, recyclability, improved solvation ability, low volatility, and thermal stability. These have been at the forefront of the most innovative fields of science and technology during the past few years. ILs may be employed in new drug formulation development and drug design in the field of pharmacy for various functions such as improvement of solubility, targeted drug delivery, stabilizer, permeability enhancer, or improvement of bioavailability in the development of pharmaceutical or vaccine dosage formulations. Ionic liquids have become a key component in various areas such as synthetic and catalytic chemistry, extraction, analytics, biotechnology, etc., due to their superior abilities along with highly modifiable potential. This study concentrates on the usage of ILs in various pharmaceutical applications enlisting their numerous purposes from the delivery of drugs to pharmaceutical synthesis. To better comprehend cuttingedge technologies in IL-based drug delivery systems, highly focused mechanistic studies regarding the synthesis/preparation of ILs and their biocompatibility along with the ecotoxicological and biological effects need to be studied. The use of IL techniques can address key issues regarding pharmaceutical preparations such as lower solubility and bioavailability which plays a key role in the lack of effectiveness of significant commercially available drugs.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1197-1210"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41184722","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Recent Updates in Inhalable Drug Delivery System against Various Pulmonary Diseases: Challenges and Future Perspectives.","authors":"Kabi Raj Chaudhary, Karanvir Singh, Charan Singh","doi":"10.2174/0115672018265571231011093546","DOIUrl":"10.2174/0115672018265571231011093546","url":null,"abstract":"<p><p>In the current scenario, pulmonary disease has become a prime burden for morbidity and mortality alongside tremendous social and economic crises throughout the world. Numerous conventional drug delivery system and treatment approach targeting the respiratory region has been driven out. However, effective and accurate recovery has not been achieved yet. In this regard, nanotechnological- based inhalable drug delivery strategy including polymeric, lipidic, or metallic-based respirable microparticles plays an indispensable role in circumventing numerous challenges faced during traditional treatment. Excellent aerodynamic performance leads to enhanced lung targetability, reduced dosing frequency and hence systemic toxicities, as well as improved pharmaceutical attributes, and therefore pharmacokinetic profiles are interminable factors associated with nanotechnologicalbased inhalable delivery. In this review, we comprehensively explored recent advancements in nanotechnologically engineered inhalable formulations targeting each of the mentioned pulmonary diseases. Moreover, we systematically discussed possible respiratory or systemic toxicities about the indeterminate and undefined physicochemical characteristics of inhaled particles.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1320-1345"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49695728","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sudipta Das, Baishali Ghosh, Rudra Narayan Sahoo, Amit Kumar Nayak
{"title":"Recent Advancements in Bioelectronic Medicine: A Review.","authors":"Sudipta Das, Baishali Ghosh, Rudra Narayan Sahoo, Amit Kumar Nayak","doi":"10.2174/0115672018286832231218112557","DOIUrl":"10.2174/0115672018286832231218112557","url":null,"abstract":"<p><p>Bioelectronic medicine is a multidisciplinary field that combines molecular medicine, neurology, engineering, and computer science to design devices for diagnosing and treating diseases. The advancements in bioelectronic medicine can improve the precision and personalization of illness treatment. Bioelectronic medicine can produce, suppress, and measure electrical activity in excitable tissue. Bioelectronic devices modify specific neural circuits using electrons rather than pharmaceuticals and uses of bioelectronic processes to regulate the biological processes underlining various diseases. This promotes the potential to address the underlying causes of illnesses, reduce adverse effects, and lower costs compared to conventional medication. The current review presents different important aspects of bioelectronic medicines with recent advancements. The area of bioelectronic medicine has a lot of potential for treating diseases, enabling non-invasive therapeutic intervention by regulating brain impulses. Bioelectronic medicine uses electricity to control biological processes, treat illnesses, or regain lost capability. These new classes of medicines are designed by the technological developments in the detection and regulation of electrical signaling methods in the nervous system. Peripheral nervous system regulates a wide range of processes in chronic diseases; it involves implanting small devices onto specific peripheral nerves, which read and regulate the brain signaling patterns to achieve therapeutic effects specific to the signal capacity of a particular organ. The potential for bioelectronic medicine field is vast, as it investigates for treatment of various diseases, including rheumatoid arthritis, diabetes, hypertension, paralysis, chronic illnesses, blindness, etc.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1445-1459"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139089844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sindi P Ndlovu, Sibusiso Alven, Kula Hlalisa, Blessing A Aderibigbe
{"title":"Cellulose Acetate-Based Wound Dressings Loaded with Bioactive Agents: Potential Scaffolds for Wound Dressing and Skin Regeneration.","authors":"Sindi P Ndlovu, Sibusiso Alven, Kula Hlalisa, Blessing A Aderibigbe","doi":"10.2174/0115672018262616231001191356","DOIUrl":"10.2174/0115672018262616231001191356","url":null,"abstract":"<p><p>Wound healing and skin regeneration are major challenges in chronic wounds. Among the types of wound dressing products currently available in the market, each wound dressing material is designed for a specific wound type. Some of these products suffer from various shortcomings, such as poor antibacterial efficacy and mechanical performance, inability to provide a moist environment, poor permeability to oxygen and capability to induce cell migration and proliferation during the wound healing process. Hydrogels and nanofibers are widely reported wound dressings that have demonstrated promising capability to overcome these shortcomings. Cellulose acetate is a semisynthetic polymer that has attracted great attention in the fabrication of hydrogels and nanofibers. Loading bioactive agents such as antibiotics, essential oils, metallic nanoparticles, plant extracts, and honey into cellulose acetate-based nanofibers and hydrogels enhanced their biological effects, including antibacterial, antioxidant, and wound healing. This review reports cellulose acetate-based hydrogels and nanofibers loaded with bioactive agents for wound dressing and skin regeneration.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1226-1240"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41242872","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Novel Biomaterials Based Strategies for Neurodegeneration: Recent Advancements and Future Prospects.","authors":"Dilpreet Singh, Sanjay Nagdev","doi":"10.2174/0115672018275382231215063052","DOIUrl":"10.2174/0115672018275382231215063052","url":null,"abstract":"<p><p>Neurodegenerative diseases, including Alzheimer's disease, Parkinson's disease, and Huntington's disease, pose significant challenges for effective treatment due to the complex nature of the central nervous system and the limited delivery of therapeutic agents to the brain. Biomaterial-based drug delivery systems offer promising strategies to overcome these challenges and improve therapeutic outcomes. These systems utilize various biomaterials, such as nanoparticles, hydrogels, and implants, to deliver drugs, genes, or cells to the affected regions of the brain. They provide advantages such as targeted delivery, controlled release, and protection of therapeutic agents. This review examines the role of biomaterials in drug delivery for neurodegeneration, discussing different biomaterialbased approaches, including surface modification, encapsulation, and functionalization techniques. Furthermore, it explores the challenges, future perspectives, and potential impact of biomaterialbased drug delivery systems in the field of neurodegenerative diseases.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1037-1049"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139682293","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Qiuting Guo, Xuan Wang, Yao Wang, Peijie Zhou, Xiaofei Zhang
{"title":"Volatile Oil of <i>Magnolia biondii</i> Pamp. for Transnasal Administration: Its Preparation, Characterization, and Mechanism of Action in the Treatment of Allergic Rhinitis.","authors":"Qiuting Guo, Xuan Wang, Yao Wang, Peijie Zhou, Xiaofei Zhang","doi":"10.2174/0115672018286048240229180813","DOIUrl":"10.2174/0115672018286048240229180813","url":null,"abstract":"<p><strong>Background: </strong>Allergic Rhinitis (AR) is a common chronic nasal condition usually caused by allergens. The immune system overreacts when the body is exposed to allergens, releasing a lot of tissue chemicals that cause congestion, more secretions, and an inflammatory reaction in the nasal mucosa.</p><p><strong>Method: </strong>In clinical practice, it remains a significant public health issue. Modern pharmacological studies have demonstrated that Magnolia Volatile Oil (MVO) has good anti-inflammatory, antibacterial, immunomodulatory, and other pharmacological effects. Previous research and literature reports have reported that MVO has good therapeutic effects on allergic rhinitis. However, due to the poor water solubility of Magnolia, its bioavailability is low. The purpose of this present work is to develop a new microemulsion formulation to improve the stability and bioavailability of MVO.</p><p><strong>Results: </strong>The droplet size, PDI, and zeta potential of Magnolia volatile oil microemulsion (MVOME) were characterized along with its physical characteristics, and these values were found to be 14.270.03 nm, 0.09410.31, and -0.35850.12 mV, respectively, demonstrating the successful formation of microemulsion. In OVA-induced AR rats, MVO-ME dramatically reduced the serum levels of TNF-α, IL-1β, and IL-6 inflammatory factors. In addition, MVO-ME significantly inhibited the expression of protein levels of PPAR-γ and P65 in the nasal mucosa of AR rats. In this regard, we hypothesized that MVO-ME may play a therapeutic role in AR by activating the PPAR signaling pathway as well as inhibiting the activation of the NF/κB signaling pathway.</p><p><strong>Conclusion: </strong>MVO-ME has systematic advantages, such as high solubility, bioavailability, etc. It is expected to be an efficient nano-drug delivery system for the clinical treatment of allergic rhinitis.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1408-1421"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140029961","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Nanostructured Lipid Carrier-Mediated Transdermal Delivery System of Glibenclamide for Gestational Diabetes: Pharmacokinetic and Pharmacodynamic Evaluation.","authors":"M Ashwini, Preethi Sudheer, Bharani S Sogali","doi":"10.2174/0115672018274038231212105440","DOIUrl":"10.2174/0115672018274038231212105440","url":null,"abstract":"<p><strong>Background: </strong>Gestational diabetes mellitus (GDM) poses significant risks during pregnancy for both mother and fetus. Adherence to oral antidiabetic medications, like glibenclamide (GB), can be challenging, necessitating novel drug delivery methods. Nanostructured lipid carriers (NLC) offer a promising approach by efficiently permeating the skin due to their small size and lipid-based composition.</p><p><strong>Objective: </strong>This study aimed to develop and evaluate transdermal patches loaded with glibenclamide NLCs to treat GDM.</p><p><strong>Methods: </strong>Glibenclamide NLCs were prepared using hot homogenization with ultrasonication and melt dispersion method. A central composite design was utilized to optimize the formulations. Transdermal patches containing optimized NLCs were developed using HPMC K 100 and Eudragit L polymers. The patches were evaluated for various parameters, and their pharmacokinetic and pharmacodynamic studies were carried out to assess their safety and efficacy.</p><p><strong>Results: </strong>Optimized NLCs efficiently permeated rat skin. Cell viability studies indicated the nontoxicity of the formulations. NLC-loaded transdermal patches (F2 and F7) showed drug release of 1098 μg/cm<sup>2</sup> and 1001.83 μg/cm<sup>2</sup> in 24 h, with a 2.5-fold higher flux and permeation coefficient than the GB patch. Pharmacokinetic analysis revealed Tmax of 8 and 10 h and C<sub>max</sub> of 7127 ng/ml and 7960 ng/ml for F2 and F7, respectively, ensuring sustained drug action. AUC0-α was 625681 ng/ml·h and 363625 ng/ml·h for F2 and F7, respectively, indicating improved bioavailability.</p><p><strong>Conclusion: </strong>Transdermal patches incorporating NLCs hold promise for enhancing glibenclamide's therapeutic efficacy in GDM treatment. Improved skin permeation, sustained drug release, and enhanced bioavailability make NLC-based transdermal patches a potential alternative with better patient compliance.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1386-1407"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139428217","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Teng Wei, Bing-Yu Zhou, Xin-Hong Wu, Xue-Ai Liu, Ming-Wei Huo, Xiang-Xiang Huang, Ling-Zhi Shi, Li-Li Shi, Qin-Ri Cao
{"title":"Development of Polyvinyl Alcohol/Polyethylene Glycol Copolymer-based Orodispersible Films Loaded with Entecavir: Formulation and <i>In vitro</i> Characterization.","authors":"Teng Wei, Bing-Yu Zhou, Xin-Hong Wu, Xue-Ai Liu, Ming-Wei Huo, Xiang-Xiang Huang, Ling-Zhi Shi, Li-Li Shi, Qin-Ri Cao","doi":"10.2174/0115672018261294231024093926","DOIUrl":"10.2174/0115672018261294231024093926","url":null,"abstract":"<p><strong>Purpose: </strong>The aim of the study is to prepare entecavir (ETV)-loaded orodispersible films (ODFs) using polyvinyl alcohol (PVA)/polyethylene glycol (PEG) graft copolymer (Kollicoat® IR) as a film-forming agent, and further to evaluate the dissolution rate, mechanical and physicochemical properties of films.</p><p><strong>Methods: </strong>ETV-ODFs were prepared by a solvent casting method. The amount of film-forming agent, plasticizer, and disintegrating agent was optimized in terms of the appearance, thickness, disintegration time and mechanical properties of ODFs. The compatibility between the drug and each excipient was conducted under high temperature (60 °C), high humidity (RH 92.5%), and strong light (4500 Lx) for 10 days. The dissolution study of optimal ODFs compared with the original commercial tablet (Baraclude®) was performed using a paddle method in pH 1.0, pH 4.5, pH 6.8, and pH 7.4 media at 37 °C. The morphology of ODFs was observed via scanning electron microscopy (SEM). The mechanical properties such as tensile strength (TS), elastic modulus (EM), and percentage elongation (E%) of ODFs were evaluated using the universal testing machine. The physicochemical properties of ODFs were investigated using X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR).</p><p><strong>Results: </strong>The related substances were less than 0.5% under high temperature, high humidity, and strong light for 10 days when ETV was mixed with excipients. The optimal formulation of ODFs was set as the quality ratio of Kollicoat® IR, glycerol, sodium alginate (ALG-Na): TiO2: MCC+CMC-Na: ETV was 60:9:12:1:1:1. The drug-loaded ODFs were white and translucent with excellent stripping property. The thickness, disintegration time, EM, TS, and E% were 103.33±7.02 μm, 25.31±1.95 s, 25.34±8.69 Mpa, 2.14±0.26 Mpa, and 65.45±19.41 %, respectively. The cumulative drug release from ODFs was more than 90% in four different media at 10 min. The SEM showed that the drug was highly dispersible in ODFs, and the XRD, DSC, and FT-IR results showed that there occurred some interactions between the drug and excipients.</p><p><strong>Conclusion: </strong>In conclusion, the developed ETV-loaded ODFs showed relatively short disintegration time, rapid drug dissolution, and excellent mechanical properties. This might be an alternative to conventional ETV Tablets for the treatment of chronic hepatitis B.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1362-1374"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71490869","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jiayan Liu, Song Guo, Shuai Hong, Jingshu Piao, Mingguan Piao
{"title":"Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: <i>In vitro</i> Characterization and <i>In vivo</i> Evaluation.","authors":"Jiayan Liu, Song Guo, Shuai Hong, Jingshu Piao, Mingguan Piao","doi":"10.2174/0115672018279370240103062944","DOIUrl":"10.2174/0115672018279370240103062944","url":null,"abstract":"<p><strong>Background: </strong>Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.</p><p><strong>Objective: </strong>The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.</p><p><strong>Methods: </strong>Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.</p><p><strong>Results: </strong>The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.</p><p><strong>Conclusion: </strong>These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":"1537-1547"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139514473","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}