Recent advances in drug delivery and formulation最新文献

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Application of D-Optimal Mixture Design in the Development of Nanocarrier-Based Darifenacin Hydrobromide Gel. d -最优混合物设计在纳米载体氢溴酸达利那新凝胶制备中的应用。
Recent advances in drug delivery and formulation Pub Date : 2023-01-01 DOI: 10.2174/2667387817666230221141501
Divya Patel, Maanika Menon, Pranav Shah, Meenakshi Patel, Manisha Lalan
{"title":"Application of D-Optimal Mixture Design in the Development of Nanocarrier-Based Darifenacin Hydrobromide Gel.","authors":"Divya Patel, Maanika Menon, Pranav Shah, Meenakshi Patel, Manisha Lalan","doi":"10.2174/2667387817666230221141501","DOIUrl":"https://doi.org/10.2174/2667387817666230221141501","url":null,"abstract":"BACKGROUND Darifenacin hydrobromide, a BCS Class II drug, is poorly bioavailable due to extensive first-pass metabolism. The present study is an attempt to investigate an alternative route of drug delivery by developing a nanometric microemulsion-based transdermal gel for the management of an overactive bladder. METHOD Oil, surfactant, and cosurfactant were selected based on the solubility of the drug, and surfactant: cosurfactant in surfactant mixture (Smix) was selected at a 1:1 ratio as inferred from the pseudo ternary phase diagram. The D-optimal mixture design was used to optimize the o/w microemulsion wherein the globule size and zeta potential were selected as dependable variables. The prepared microemulsions were also characterized for various physico-chemical properties like transmittance, conductivity, and TEM. The optimized microemulsion was gelled using Carbopol 934 P and assessed for drug release in-vitro and ex-vivo, viscosity, spreadability, pH, etc. Results: Drug excipient compatibility studies showed that the drug was compatible with formulation components. The optimized microemulsion showed a globule size of less than 50 nm and a high zeta potential of -20.56 mV. The ME gel could sustain the drug release for 8 hours as reflected in in-vitro and ex-vivo skin permeation and retention studies. The accelerated stability study showed no significant change in applied storage conditions. CONCLUSION An effective, stable, non-invasive microemulsion gel containing darifenacin hydrobromide was developed. The achieved merits could translate into increased bioavailability and dose reduction. Further confirmatory in-vivo studies on this novel formulation, which is a cost-effective & industrially scalable option, can improve the pharmacoeconomics of overactive bladder management.","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9778302","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}
引用次数: 0
Biodegradable Polymer-Based Microspheres for Depot Injection-Industry Perception. 仓库注射用可生物降解聚合物基微球-工业感知。
Recent advances in drug delivery and formulation Pub Date : 2023-01-01 DOI: 10.2174/2667387817666230119103126
Anand Kyatanwar, Mangal Nagarsenker, Bala Prabhakar
{"title":"Biodegradable Polymer-Based Microspheres for Depot Injection-Industry Perception.","authors":"Anand Kyatanwar,&nbsp;Mangal Nagarsenker,&nbsp;Bala Prabhakar","doi":"10.2174/2667387817666230119103126","DOIUrl":"https://doi.org/10.2174/2667387817666230119103126","url":null,"abstract":"<p><p>The discovery of proteins and peptides marked the actual beginning for pharmaceutical companies to do research on novel delivery systems for delivering these therapeutic proteins. Biodegradable polymer-based microspheres for controlled-release depot injection are known for decades and have proved to be one of the best possible approaches. Despite being known for decades, the commercial success of microsphere-based delivery systems remains limited. Very few products are seen in the market with no generics available for approved brand products whose patents have either expired or are about to expire. All this points to the complexities involved in developing these delivery systems. Still, many hurdles remain in developing these drug delivery systems namely, poor drug entrapment, unwanted burst release, poor in vitro in vivo correlation, lack of proper in vitro testing methods, problems involved during scale-up, and the most important hurdle being sterilization of the product. To achieve successful product development, all of these technical difficulties need to be simultaneously dealt with and resolved. This article attempts to highlight the problem areas for these delivery systems along with the regulatory requirements involved and map the present status of these delivery systems.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9789791","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}
引用次数: 0
Advances in Pharmacokinetic Modelling and Computational Approaches for Nanoparticles in Drug Delivery Systems. 纳米颗粒给药系统药代动力学建模与计算方法研究进展。
Recent advances in drug delivery and formulation Pub Date : 2023-01-01 DOI: 10.2174/2667387817666230907093403
Shivang Dhoundiyal, Md Aftab Alam
{"title":"Advances in Pharmacokinetic Modelling and Computational Approaches for Nanoparticles in Drug Delivery Systems.","authors":"Shivang Dhoundiyal, Md Aftab Alam","doi":"10.2174/2667387817666230907093403","DOIUrl":"10.2174/2667387817666230907093403","url":null,"abstract":"<p><p>Generally, therapeutic drugs have issues like poor solubility, rapid removal from the bloodstream, lack of targeting, and an inability to translocate across cell membranes. Some of these barriers can be overcome by using nano drug delivery systems (DDS), which results in more efficient drug delivery to the site of action. Due to their potential application as drug delivery systems, nanoparticles are the main topic of discussion in this article. Experimental and computational investigations have substantially aided in the understanding of how nanocarriers work and how they interact with medications, biomembranes and other biological components. This review explores how computational modelling can aid in the rational design of DDS that has been optimized and improved upon. The most commonly used simulation methods for studying DDS and some of the most important biophysical elements of DDS are also discussed. Then, we conclude by investigating the computational properties of various types of nanocarriers, such as dendrimers and dendrons, polymer-, peptide-, nucleic acid-, lipid-, carbon-based DDS, and gold nanoparticles.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10553840","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}
引用次数: 0
Meet the Co-Editor 与合作编辑见面
Recent advances in drug delivery and formulation Pub Date : 2022-12-01 DOI: 10.2174/266738781604221222090130
W. Wui
{"title":"Meet the Co-Editor","authors":"W. Wui","doi":"10.2174/266738781604221222090130","DOIUrl":"https://doi.org/10.2174/266738781604221222090130","url":null,"abstract":"","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73091747","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}
引用次数: 0
Fabrication and In Vitro Evaluation of Febuxostat Tablet for Obtaining Biphasic Drug Release Profile. 制作非布索坦片剂并对其进行体外评估,以获得双相药物释放谱。
Recent advances in drug delivery and formulation Pub Date : 2022-11-16 DOI: 10.2174/2667387817666221116100127
Dipika Chavda, Deepika Joshi, Vaishali Thakkar, Tejal Gandhi
{"title":"Fabrication and In Vitro Evaluation of Febuxostat Tablet for Obtaining Biphasic Drug Release Profile.","authors":"Dipika Chavda, Deepika Joshi, Vaishali Thakkar, Tejal Gandhi","doi":"10.2174/2667387817666221116100127","DOIUrl":"10.2174/2667387817666221116100127","url":null,"abstract":"<p><p>Aim and Objective The primary aim of the present investigation was to adopt the concept of quality by design (QbD) for developing Febuxostat matrix tablets containing a novel combination of polyethylene oxide (PEO), pre-gelatinized starch (PGS) and lactose for obtaining biphasic drug release. Experimental work Febuxostat-containing matrix tablets were prepared by direct compression using 32 full factorial designs. The tablets were prepared with varying amounts of PEO WSR 301 to PGS and lactose to obtain the desired release pattern. The chosen responses were cumulative % drug released at 1, 6 and 12 hours. The evaluation of tablets was done for pre and post-compressional parameters. Compared with the marketed tablet, the optimized formulations were selected based on in vitro drug release. Dose dumping was checked in the dissolution medium containing up to 40% alcohol. Result and discussion The results of the dissolution study indicated that the batch containing a 1:1 ratio of PEO WSR 301 and PGS (15 mg each) and 20 mg of Lactose showed fast initial drug release to imitate the pharmacological action followed by sustained drug release effect. The use of Lactose facilitated immediate drug release, while PEO WSR 301 and PGS exhibited the opposite effect on cumulative drug release. The results of the 32 Factorial design revealed that the concentration of Lactose is a critical parameter. Dose dumping was not observed in the alcoholic dissolution medium. Kinetic equations were fitted to the dissolution data after 1 hour of the dissolution study. Conclusion The type (soluble or swellable) and the concentration of excipients (low or high) dictate the tablets' drug release. The study's outcome revealed that the most critical material attribute is the amount of lactose. The novel combination of PEO, PGS and lactose can bypass existing patents and give more industrial applicability.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40475308","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}
引用次数: 0
Doxorubicin Loaded Gold Nanoparticles Mitigate Liver Fibrosis and Inflammatory Cytokines Gene Expression in Rat. 负载多柔比星的金纳米粒子可减轻大鼠肝纤维化和炎症细胞因子基因表达
Recent advances in drug delivery and formulation Pub Date : 2022-10-20 DOI: 10.2174/2667387817666221020090050
Yasmeen Ishaq, Hamna Naeem, Sana Khurshid, Rabia Tabbasam, Zeeshan Haider
{"title":"Doxorubicin Loaded Gold Nanoparticles Mitigate Liver Fibrosis and Inflammatory Cytokines Gene Expression in Rat.","authors":"Yasmeen Ishaq, Hamna Naeem, Sana Khurshid, Rabia Tabbasam, Zeeshan Haider","doi":"10.2174/2667387817666221020090050","DOIUrl":"10.2174/2667387817666221020090050","url":null,"abstract":"<p><strong>Background: </strong>Gold nanoparticles have the potential to be used as a carrier in drug delivery system due to their small size, large surface area and short circulation time in blood.</p><p><strong>Objective: </strong>This study aims that doxorubicin conjugation with gold nanoparticles (AuNPs) may reduce its toxicity as well as improve therapeutic efficacy.</p><p><strong>Methods: </strong>Five groups of Albino rats were used; 1: healthy control, 2: Injured, 3: injured and treated with Dox, 4: Injured and treated with AuNPs, 5: Injured and treated with AuNPs: Dox. At the end of the experiment, blood and liver tissues were processed for biochemical and histopathological analysis. The expression of collagen, HO-1, IL-6 and TNF-α genes involved in liver fibrosis was observed through real-time PCR.</p><p><strong>Results: </strong>At the end of the experiment, it was observed that the body weights of DOX treated rats decreased by 0.72%, however, AuNPs and Au: DOX treated rats were 15.3% and 29.13% respectively. The percentage of liver protection determined through alanine aminotransferase and aspartate aminotransferase levels in DOX, AuNPs and AuNPs: DOX treated groups were 39.21%, 79.26%, 98.17% and 47.77%, 84.17%, 97.92% respectively. That represents better recovering liver in Dox-AuNPs treated rats compared to others. Histopathological and gene expression studies further support the findings. The mRNA expression levels of inflammatory and oxidative stress related genes HO-1, IL-6 and TNF-α were upregulated in the injured group but downregulated in the treated group.</p><p><strong>Conclusion: </strong>As depicted through biochemical, histopathological and gene expression studies, Au: DOX conjugate group seems to be protective against liver fibrosis.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40677606","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}
引用次数: 0
In situ Hydrogels for Effective Treatment of Cancer: Strategies and Polymers Used. 有效治疗癌症的原位水凝胶:使用的策略和聚合物。
Recent advances in drug delivery and formulation Pub Date : 2022-10-05 DOI: 10.2174/2667387816666221005102931
Anshula Mehra, Abhay Tharmatt, Navdeep Saini, Gurdeep Singh, Kirandeep Kaur, Gurpreet Singh, Neena Bedi
{"title":"In situ Hydrogels for Effective Treatment of Cancer: Strategies and Polymers Used.","authors":"Anshula Mehra, Abhay Tharmatt, Navdeep Saini, Gurdeep Singh, Kirandeep Kaur, Gurpreet Singh, Neena Bedi","doi":"10.2174/2667387816666221005102931","DOIUrl":"10.2174/2667387816666221005102931","url":null,"abstract":"<p><p>Cancer is a worldwide health ailment with no known boundaries in terms of mortality and occurrence rates, thus is one of the biggest threats to humankind. Hence, there is an absolute need to develop novel therapeutics to bridge the infirmities associated with chemotherapy and conventional surgical methodologies including impairment of normal tissue, compromised drug efficiency and an escalation in side effects. In lieu of this, there's been a surge in curiosity towards development of injectable hydrogels for cancer therapy because local administration of the active pharmaceutical agent offers encouraging advantages such as providing higher effective dose at target site, prolonged retention time of drug, ease of administration, mitigation of dose in vivo ,improved patient compliance. Furthermore, due to its biocompatible nature such systems can significantly reduce the side effects that occur on long-term exposure to chemotherapy. The present review details the most recent advancements in in-situ gel forming polymers (natural and synthetic), polymeric cross-linking methodologies and in-situ gelling mechanisms, focusing on their clinical benefits in cancer therapy.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33507049","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}
引用次数: 0
Recent advancements on hyperthermia driven controlled drug delivery from nanotherapeutics. 纳米疗法在热疗驱动可控给药方面的最新进展。
Recent advances in drug delivery and formulation Pub Date : 2022-09-02 DOI: 10.2174/2667387816666220902091043
Mirza Shahed Baig, M Akiful Haque, Teja Kumar Reddy Konatham, Badrud Duza Mohammad, Barrawaz Aateka Yahya, Shaikh Sana Saffiruddin, Falak A Siddiqui, Sharuk L Khan
{"title":"Recent advancements on hyperthermia driven controlled drug delivery from nanotherapeutics.","authors":"Mirza Shahed Baig, M Akiful Haque, Teja Kumar Reddy Konatham, Badrud Duza Mohammad, Barrawaz Aateka Yahya, Shaikh Sana Saffiruddin, Falak A Siddiqui, Sharuk L Khan","doi":"10.2174/2667387816666220902091043","DOIUrl":"10.2174/2667387816666220902091043","url":null,"abstract":"<p><p>Previous reviews of the works on magnetic nanoparticles for hyperthermia induced treatment concentrated mostly on magnetic fluid hyperthermia (MFH) employing monometallic/metal oxide nanocomposites. In the literature, the word \"hyperthermia\" was also limited to the use of heat for medicinal purposes. A number of publications have recently been published demonstrating that magnetic nanoparticle-based hyperthermia may produce restricted high temperatures, resulting in the release of medicines that are either connected to the magnetic nanoparticles or encased in polymer matrices. In this debate, we propose broadening the concept of \"hyperthermia\" to encompass temperature-based treatment as well as magnetically controlled medication delivery. The review also addresses core-shell magnetic nanomaterials, particularly nanoshells made by stacked assembly, for the use of hyperthermia-based treatment and precise administration of drugs. The primary objective of this review article is to demonstrate how the combination of hyperthermia-induced therapy and 'on demand' drug release models may lead to effective applications in personalized medicine.</p>","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40345801","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}
引用次数: 0
Exploring the patent landscape and innovation of hydrogel-based bioinks used for 3D bioprinting. 探索用于3D生物打印的水凝胶生物墨水的专利景观和创新。
Recent advances in drug delivery and formulation Pub Date : 2022-04-29 DOI: 10.2174/2667387816666220429095834
A. Fatimi
{"title":"Exploring the patent landscape and innovation of hydrogel-based bioinks used for 3D bioprinting.","authors":"A. Fatimi","doi":"10.2174/2667387816666220429095834","DOIUrl":"https://doi.org/10.2174/2667387816666220429095834","url":null,"abstract":"BACKGROUND\u0000This paper provides a comprehensive overview of the patent situation for hydrogel-based bioinks used for 3D bioprinting globally. It encapsulates information which could be used as a reference by researchers in the fields of 3D bioprinting, biomaterials, tissue engineering, and biomedical engineering, as well as those interested in biomaterials, especially in the formulation of hydrogels. It can also inform policy discussions, strategic research planning, or technology transfer in this area. The findings presented hereinafter are considered novel research aspects regarding the used hydrogels, their preparation methods, and their formulations, as well as the 3D bioprinting process using hydrogels. Furthermore, the novel part, synthesized patents, is regarded as a breakthrough in hydrogel-based bioinks.\u0000\u0000\u0000METHODS\u0000The following research aspects of this study are based on data collection from selected patent databases. The search results are then analyzed according to publication years, classification, inventors, applicants, and owners, as well as jurisdictions.\u0000\u0000\u0000RESULTS\u0000Based on the earliest priority date, it is possible to precisely assume that 2004 is considered the starting year of patenting of hydrogel-based bioinks. Furthermore, 2020 was the year with the most patent documents. According to the findings, the United States, China, and the Republic of Korea are the most prolific countries in terms of patenting on hydrogel-based bioinks. The most prolific patenting companies are from the United States, Sweden, and Australia, while universities from the Republic of Korea and the United States are the academic institutions leading the way. Most inventions of hydrogel-based bioinks intended for hydrogels or hydrocolloids used as materials for prostheses or for coating prostheses are characterized by their function or physical properties.\u0000\u0000\u0000CONCLUSION\u0000The state has been reviewed by introducing what has been patented concerning hydrogel-based bioinks. Knowledge clusters and expert driving factors indicate that the research based on biomaterials, tissue engineering, and biofabrication is concentrated in the most common patent documents. Finally, this paper, which gives a competitive analysis of the past, present, and future trends in hydrogel-based bioinks, leads to various recommendations that could help one to plan and innovate research strategies.","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77032041","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}
引用次数: 13
Formulation development of Azadirachta indica extract as nanosuppositories improves its intrarectal delivery for the treatment of malaria. 印楝提取物纳米栓剂的配方开发改善了其直肠内给药治疗疟疾的效果。
Recent advances in drug delivery and formulation Pub Date : 2022-04-26 DOI: 10.2174/2667387816666220426134156
Tochukwu C. Okeke, C. Umeyor, I. Nzekwe, I. C. Umeyor, N. Nebolisa, E. Uronnachi, C. Nwakile, Chizoba Austinline Ekweogu, O. Aziakpono, A. Attama
{"title":"Formulation development of Azadirachta indica extract as nanosuppositories improves its intrarectal delivery for the treatment of malaria.","authors":"Tochukwu C. Okeke, C. Umeyor, I. Nzekwe, I. C. Umeyor, N. Nebolisa, E. Uronnachi, C. Nwakile, Chizoba Austinline Ekweogu, O. Aziakpono, A. Attama","doi":"10.2174/2667387816666220426134156","DOIUrl":"https://doi.org/10.2174/2667387816666220426134156","url":null,"abstract":"BACKGROUND\u0000Previous folkloric and experimental reports have demonstrated the antimalarial efficacy of Azadirachta indica (AZA) extracts. However, one of the major challenges facing its application for the clinical treatment of malaria is the design of an acceptable dosage form.\u0000\u0000\u0000OBJECTIVE\u0000Consequently, we developed AZA extract-loaded nanostructured lipid carriers (NLC) for the formulation of suppositories, denoted as nanosuppositories, for intrarectal treatment of malaria.\u0000\u0000\u0000METHODS\u0000Various batches of NLC-bearing AZA extract were formulated based on lipid matrices prepared using graded concentrations of Softisan®154 and Tetracarpidium conophorum or walnut oil. NLC was investigated by size, and differential scanning calorimetry (DSC). Suppository bearing AZA extract-loaded NLC was developed using cocoa butter or theobroma oil, and their physicochemical properties were profiled. In vitro drug release and in vivo antimalarial (using Plasmodium berghei-infected mice) evaluation were investigated.\u0000\u0000\u0000RESULTS\u0000NLCs had sizes in nanometer scale ranging from 329.5 - 806.0 nm, and were amorphized as shown by DSC thermograms. Nanosuppositories were torpedo- or bullet- shaped, weighed 138 - 368 mg, softened/liquefied between 4.10 - 6.92 min, and had controlled release behaviour. In vivo antimalarial study revealed excellent antimalarial efficacy of the nanosuppositories comparable with a commercial brand (Plasmotrim®) and better than the placebo (unloaded nanosuppository), and without toxic alterations of hepatic and renal biochemical factors.\u0000\u0000\u0000CONCLUSION\u0000Thus, AZA extract could be rationally loaded in nanostructured lipid carriers (NLC) for further development as nanosuppositories and deployed as an effective alternative with optimum convenience for intrarectal treatment of malaria.","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85570022","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}
引用次数: 0
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