Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 73
Filtrar
1.
Mol Biol Rep ; 51(1): 82, 2024 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-38183502

RESUMO

In today's culture, obesity and overweight are serious issues that have an impact on how quickly diabetes develops and how it causes complications. For the development of more effective therapies, it is crucial to understand the molecular mechanisms underlying the chronic problems of diabetes. The most prominent effects of diabetes are microvascular abnormalities such as retinopathy, nephropathy, and neuropathy, especially diabetes foot ulcers, as well as macrovascular abnormalities such as heart disease and atherosclerosis. MicroRNAs (miRNAs), which are highly conserved endogenous short non-coding RNA molecules, have been implicated in several physiological functions recently, including the earliest stages of the disease. By binding to particular messenger RNAs (mRNAs), which cause mRNA degradation, translation inhibition, or even gene activation, it primarily regulates posttranscriptional gene expression. These molecules exhibit considerable potential as diagnostic biomarkers for disease and are interesting treatment targets. This review will provide an overview of the latest findings on the key functions that miRNAs role in diabetes and its complications, with an emphasis on the various stages of diabetic wound healing.


Assuntos
Aterosclerose , Diabetes Mellitus , Pé Diabético , Cardiopatias , MicroRNAs , Humanos , Pé Diabético/genética , Pé Diabético/terapia , Úlcera , MicroRNAs/genética , RNA Mensageiro
2.
Biomed Chromatogr ; 38(4): e5815, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38128133

RESUMO

The current research involved the development and validation of an easy, cost-effective, and sensitive bioanalytical reverse-phase high-performance liquid chromatography method for the assessment of palbociclib (PAL) in rat plasma and kidney, liver, spleen and heart. A response surface methodology-based Box-Behnken design was used to optimize critical chromatographic conditions such as buffer pH, organic phase concentration and flow rate to attain good sensitivity, tailing factor and retention time. The conditions were: pH of buffer, 4.5; organic phase concentration, 40%; Shimpac column with 1.0 ml/min flow rate. The responses were: tailing factor, 1.29 ± 0.03, sensitivity, 366,593 ± 8,592; and retention time, 4.5 ± 0.05 min. The samples were extracted by a protein precipitation method, and absolute recoveries were in the range of 88.99-95.08%. The linearity of the developed method was validated over the range 100-2,000 ng/ml (r2 ≥ 0.994) in all tested matrices. The developed bioanalytical method showed greater accuracy (0.98 and 4.01%) and precision (<4.88%). The method was optimized for the sensitive analysis of the PAL in rat plasma, and the kidney, liver, spleen and heart were effectively applied to pharmacokinetic studies.


Assuntos
Cromatografia de Fase Reversa , Piridinas , Ratos , Animais , Cromatografia Líquida de Alta Pressão/métodos , Piperazinas/análise
3.
Pharm Dev Technol ; 29(1): 1-12, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38015058

RESUMO

One of the most prevalent cancers affecting women globally is cervical cancer. Cervical cancer is thought to cause 570 000 new cases annually, and standard treatments can have serious side effects. In this work, the main aim is to design, fabrication, and evaluation of carboplatin loaded chitosan coated liposomal formulation (CCLF-I) for vaginal delivery in the treatment of cervical cancer. The particle size and polydispersity index of the CCLF-1 were observed at 269.33 ± 1.15 and 0.40 ± 0.002 nm, respectively. The in vitro mucin binding studies showed good adhesiveness of CCLF-I as compared to plain liposomes (CPLF-I), which was found at 23.49 and 10.80%, respectively. The ex-vivo percent drug permeation from plain liposomal formulation (CPLF-I) was found to be higher in comparison to chitosan coated liposomal formulation which was 56.33% while in CCLF-I it was observed 47.32% this is due to, higher retainability of delivery system (CCLF-I) on targeted site attained by coating of mucoadhesive polymer on liposomes. Ex vivo tissue retention studies exhibited 24.2% of CCLF-I in comparison to 10.34% from plain drug formulation (CPLF-I). The in vivo vaginal retention studies exhibited 14% of drug retention after 24 h from the novel formulation in comparison to 6% from the plain formulation. The developed CCLF-I formulation would open a new avenue in the cervical treatment.


Assuntos
Quitosana , Neoplasias do Colo do Útero , Feminino , Humanos , Lipossomos , Carboplatina , Projetos de Pesquisa , Neoplasias do Colo do Útero/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Tamanho da Partícula
4.
AAPS PharmSciTech ; 25(3): 52, 2024 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-38429601

RESUMO

As a major public health issue, colorectal cancer causes 9.4% of total cancer-related deaths and comprises 10% of new cancer diagnoses worldwide. In the year 2023, an estimated 153,020 people are expected to receive an identification of colorectal cancer (CRC), resulting in roughly 52,550 fatalities anticipated as a result of this illness. Among those impacted, approximately 19,550 cases and 3750 deaths are projected to occur in individuals under the age of 50. Irinotecan (IRN) is a compound derived from the chemical structure of camptothecin, a compound known for its action in inhibiting DNA topoisomerase I. It is employed in the treatment strategy for CRC therapies. Comprehensive in vivo and in vitro studies have robustly substantiated the anticancer efficacy of these compounds against colon cancer cell lines. Blending irinotecan in conjunction with other therapeutic cancer agents such as oxaliplatin, imiquimod, and 5 fluorouracil enhanced cytotoxicity and improved chemotherapeutic efficacy. Nevertheless, it is linked to certain serious complications and side effects. Utilizing nano-formulated prodrugs within "all-in-one" carrier-free self-assemblies presents an effective method to modify the pharmacokinetics and safety portfolio of cytotoxic chemotherapeutics. This review focuses on elucidating the mechanism of action, exploring synergistic effects, and innovating novel delivery approaches to enhance the therapeutic efficacy of irinotecan.


Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica , Neoplasias do Colo , Humanos , Irinotecano/farmacologia , Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia , Neoplasias do Colo/tratamento farmacológico , Camptotecina/farmacologia , Camptotecina/uso terapêutico , Fluoruracila/farmacologia
5.
Inflammopharmacology ; 31(1): 301-320, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36609718

RESUMO

Our main aim is in the present investigation, development and evaluation of seabuckthorn oil-based Emulgel formulation for psoriasis therapy. Anti-psoriatic activity of the SeaEmulgel was studied using Imiquimod-induced psoriasis-like inflammation model Balb/c mice and parameters such as PASI score, ear thickness, spleen to body weight index including histological staining studies, enzyme-linked immune sorbent assay (ELISA), skin compliance and safety evaluation of sea buckthorn oil was performed. The globule size and PDI of sea buckthorn oil emulsion were found to be 172.70 ± 1.73 nm and 0.117 ± 0.018, respectively. In-vivo animal studies performed on male Balb/c mice and emulgel showed a reduction in redness, scaling, inflammation in psoriasis-induced mice, which was analysed by PASI scoring, body weight, spleen weight index and ear thickness. The current investigation clearly revealed the better anti-psoriatic activity of SeaEmulgel formulation against imiquimod-induced psoriasis-like skin inflammation Balb/c mice model.


Assuntos
Psoríase , Masculino , Camundongos , Animais , Imiquimode/efeitos adversos , Pele , Inflamação/patologia , Peso Corporal , Camundongos Endogâmicos BALB C , Modelos Animais de Doenças
6.
AAPS PharmSciTech ; 24(8): 258, 2023 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-38097825

RESUMO

Even though chemotherapy stands as a standard option in the therapy of TNBC, problems associated with it such as anemia, bone marrow suppression, immune suppression, toxic effects on healthy cells, and multi-drug resistance (MDR) can compromise their effects. Nanoparticles gained paramount importance in overcoming the limitations of conventional chemotherapy. Among the various options, nanotechnology has appeared as a promising path in preclinical and clinical studies for early diagnosis of primary tumors and metastases and destroying tumor cells. PLGA has been extensively studied amongst various materials used for the preparation of nanocarriers for anticancer drug delivery and adjuvant therapy because of their capability of higher encapsulation, easy surface functionalization, increased stability, protection of drugs from degradation versatility, biocompatibility, and biodegradability. Furthermore, this review also provides an overview of PLGA-based nanoparticles including hybrid nanoparticles such as the inorganic PLGA nanoparticles, lipid-coated PLGA nanoparticles, cell membrane-coated PLGA nanoparticles, hydrogels, exosomes, and nanofibers. The effects of all these systems in various in vitro and in vivo models of TNBC were explained thus pointing PLGA-based NPs as a strategy for the management of TNBC.


Assuntos
Nanopartículas , Neoplasias de Mama Triplo Negativas , Humanos , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Ácido Láctico , Ácido Poliglicólico , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Portadores de Fármacos , Linhagem Celular Tumoral
7.
AAPS PharmSciTech ; 24(6): 157, 2023 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-37470885

RESUMO

Brinzolamide is an effective carbonic anhydrase inhibitor widely used in glaucoma therapy but limits its application due to inadequate aqueous solubility and permeability. The aim of the present research work is the development and characterization of brinzolamide-loaded ultradeformable bilosomes to enhance the corneal permeation of the drug. These ultradeformable bilosomes were prepared by ethanol injection method and evaluated for physicochemical properties, particle size, morphology, drug release, ultra-deformability, corneal permeation, and irritation potential. The optimized formulation exhibited an average particle size of 205.4 ± 2.04 nm with mono-dispersity (0.109 ± 0.002) and showed entrapment efficiency of 75.02 ± 0.017%, deformability index of 3.91, and release the drug in a sustained manner. The brinzolamide-loaded ultradeformable bilosomes released 76.29 ± 3.77% of the drug in 10 h that is 2.25 times higher than the free drug solution. The bilosomes were found non-irritant to eyes with a potential irritancy score of 0 in Hen's egg-chorioallantoic membrane assay. Brinzolamide-loaded ultradeformable bilosomes showed 83.09 ± 5.1% of permeation in 6 h and trans-corneal permeability of 8.78 ± 0.14 cm/h during the ex vivo permeation study. The acquired findings clearly revealed that the brinzolamide-loaded ultradeformable bilosomes show promising output and are useful in glaucoma therapy.


Assuntos
Inibidores da Anidrase Carbônica , Glaucoma , Animais , Feminino , Inibidores da Anidrase Carbônica/farmacologia , Galinhas , Córnea , Glaucoma/tratamento farmacológico , Tamanho da Partícula
8.
AAPS PharmSciTech ; 24(1): 46, 2023 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-36702974

RESUMO

The utility of andrographolide (AN) in visceral leishmaniasis (VL) and cutaneous leishmaniasis (CL) is limited owing to poor solubility, hindered permeation, and unstable structure under physiological conditions. The present study mainly focuses on synthesizing of andrographolide-Soya-L-α-phosphatidyl choline (ANSPC) complex in ethanol and its characterization using various spectral and analytical techniques. Results from FT-IR, 1H NMR, ROSEY, and in silico docking techniques suggest ANSPC complex formation due to inter-molecular interaction between the hydrophilic head of SPC and hydroxyl group of AN present at 24th position. ANSPC complex demonstrated the solubility of 113.93 ± 6.66 µg/mL significantly (P < 0.05) greater than 6.39 ± 0.47 µg/mL of AN. The particle size of ANSPC complex was found to be 182.2 ± 2.69 nm. The IC50 value of AN suspension (PBS, pH ~ 7.4) at 24, 48, and 72 h against Leishmania donovani (L. donovani) was noticed to be 32.76 ± 4.53, 20.87 ± 2.37, and 17.71 ± 3.06 µM/mL, respectively. Moreover, augmented aqueous solubility of ANSPC complex led to significant (P < 0.05) reduction in IC50 value, i.e., 25.02 ± 4.35, 11.31 ± 0.60, and 8.33 ± 2.71 µM/mL at 24, 48, and 72 h, respectively. The IC50 values for miltefosine were noted to be 9.84 ± 2.65, 12.13 ± 7.26, and 6.56 ± 0.61 µM/mL at similar time periods. Moreover, ANSPC complex demonstrated augmented cellular uptake at 24 h as compared to 6 h in L. donovani. We suppose that submicron size and phospholipid-mediated complexation might have endorsed the permeation of ANSPC complex across the plasma membrane of L. donovani parasite by transport mechanisms such as P-type ATPase. ANSPC complex warrants further in-depth in vivo studies under a set of stringent parameters for translating the product into a clinically viable form.


Assuntos
Leishmania donovani , Leishmaniose Visceral , Humanos , Leishmaniose Visceral/tratamento farmacológico , Leishmaniose Visceral/parasitologia , Leishmania donovani/metabolismo , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Lecitinas/metabolismo
9.
AAPS PharmSciTech ; 24(1): 50, 2023 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-36703085

RESUMO

Amongst the several nano-drug delivery systems, lipid or polymer-based core-shell nanocapsules (NCs) have garnered much attention of researchers owing to its multidisciplinary properties and wide application. NCs are structured core-shell systems in which the core is an aqueous or oily phase protecting the encapsulated drug from environmental conditions, whereas the shell can be lipidic or polymeric. The core is stabilized by surfactant/lipids/polymers, which control the release of the drug. The presence of a plethora of biocompatible lipids and polymers with the provision of amicable surface modifications makes NCs an ideal choice for precise drug delivery. In the present article, multiple lipidic and polymeric NC (LNCs and PNCs) systems are described with an emphasis on fabrication methods and characterization techniques. Far-reaching applications as a carrier or delivery system are demonstrated for oral, parenteral, nasal, and transdermal routes of administration to enhance the bioavailability of hard-to-formulate drugs and to achieve sustained and targeted delivery. This review provide in depth understanding on core-shell NC's mechanism of absorption, surface modification, size tuning, and toxicity moderation which overshadows the drawbacks of conventional approaches. Additionally, the review shines a spotlight on the current challenges associated with core-shell NCs and applications in the foreseeable future.


Assuntos
Nanocápsulas , Sistemas de Liberação de Medicamentos , Polímeros , Óleos , Disponibilidade Biológica , Portadores de Fármacos
10.
Pharm Res ; 39(11): 2761-2780, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36171346

RESUMO

PURPOSE: Cancer is one of the most common and fatal disease, chemotherapy is the major treatment against many cancer types. The anti-apoptotic BCL-2 protein's expression was increased in many cancer types and Venetoclax (VLX; BCL-2 inhibitor) is a small molecule, which selectively inhibits this specified protein. In order to increase the clinical performance of this promising inhibitor as a repurposed drug, polymeric mixed micelles formulations approach was explored. METHODS: The Venetoclax loaded polymeric mixed micelles (VPMM) were prepared by using Pluronic® F-127 and alpha tocopherol polyethylene glycol 1000 succinate (TPGS) as excipients by thin film hydration method and characteristics. The percentage drug loading capacity, entrapment efficiency and in-vitro drug release studies were performed using HPLC method. The cytotoxicity assay, cell uptake and anticancer activities were evaluated in two different cancer cells i.e. MCF-7 (breast cancer) and A-549 (lung cancer). RESULTS: Particle size, polydispersity index and zeta potential of the VPMM was found to be 72.88 ± 0.09 nm, 0.078 ± 0.009 and -4.29 ± 0.24 mV, respectively. The entrapment efficiency and %drug loading were found to be 80.12 ± 0.23% and 2.13% ± 0.14%, respectively. The IC50 of VLX was found to be 4.78, 1.30, 0.94 µg/ml at 24, 48 and 72 h, respectively in MCF-7 cells and 1.24, 0.68, and 0.314 µg/ml at 24, 48, and 72 h, respectively in A549 cells. Whereas, IC50 of VPMM was found to be 0.42, 0.29, 0.09 µg/ml at 24, 48 and 72 h, respectively in MCF-7 cells and 0.85, 0.13, 0.008 µg/ml at 24, 48 and 72 h in A549 cells, respectively, indicating VPMM showing better anti-cancer activity compared to VLX. The VPMM showed better cytotoxicity which was further proven by other assays and explained the anti-cancer activity is shown through the generation of ROS, nuclear damage,apoptotic cell death and expression of caspase-3,7, and 9 activities in apoptotic cells. CONCLUSION: The current investigation revealed that the Venetoclax loaded polymeric mixed micelles (VPMM) revealed the enhanced therapeutic efficacy against breast and lung cancer in vitro models.


Assuntos
Neoplasias Pulmonares , Micelas , Humanos , Linhagem Celular Tumoral , Polietilenoglicóis , Polímeros , Tamanho da Partícula , Proteínas Proto-Oncogênicas c-bcl-2 , Portadores de Fármacos , Vitamina E
11.
AAPS PharmSciTech ; 24(1): 26, 2022 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-36550259

RESUMO

Essential oils consist of oxygenated structures of secondary metabolites of aromatic plants with anti-psoriatic activities. Tea tree oil (TTO) is an essential oil with good anti-microbial and anti-inflammatory properties, exhibiting reduced levels of IL-1, IL-8, and PGE 2. Thymoquinone (TMQ) is popular herb in traditional medicine with known therapeutic benefits in several diseases and ailments. The ternary phase diagram was prepared with the weight ratio of Smix (Tween® 80:Labrasol®): oil:water ratio for o/w emulsion preparation. The globule size was 16.54 ± 0.13 nm, and PDI around 0.22 ± 0.01 of the TTO-TMQ emulsion and found thermodynamically stable. The percentage drug content was found in the range of 98.97 ± 0.62 to 99.45 ± 0.17% with uniformity of the ThymoGel using Carbopol®. The extensive physicochemical properties were studied using different analytical techniques, and in vitro drug release was performed using Franz-diffusion apparatus. Anti-psoriatic activity of the formulations was studied using Imiquimod-induced psoriasis-like inflammation model in male Balb/c mice and parameters like PASI score, ear thickness, and spleen to body weight index were determined as well as histological staining, ELISA, skin compliance, and safety evaluation of TTO were performed. The combination of essential oils with TMQ shows synergistic activity and efficiently reduces the psoriasis disease condition.


Assuntos
Óleos Voláteis , Psoríase , Óleo de Melaleuca , Camundongos , Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/metabolismo , Emulsões/química , Pele/metabolismo , Psoríase/metabolismo
12.
Pharm Res ; 33(7): 1769-81, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-27091032

RESUMO

PURPOSE: In the present investigation, we prepared and evaluated the paclitaxel loaded riboflavin and thiamine conjugated multi walled carbon nanotubes (PTX-Rf-MWCNTs and PTX-Tm-MWCNTs) for targeted delivery to cancer employing MCF-7 cancer cell lines. METHODS: The developed conjugates were characterized using FTIR, NMR spectroscopy, electron microscopy drug loading, release, stability, hemolytic, ex vivo and in vivo studies etc. RESULTS: The percent entrapment efficiency was found to be 87.92 ± 0.48 and 82.75 ± 0.47% of PTX-Tm-MWCNTs, PTX-Rf-MWCNTs, respectively. The percent hemolysis of purified MWCNTs, PTX-MWCNTs, PTX-Tm-MWCNTs and PTX-Rf-MWCNTs was found to be 20.49 ± 0.97, 37.39 ± 0.78, 14.61 ± 0.84 and 11.17 ± 0.77% respectively. The PTX-Tm-MWCNTs and PTX-Rf-MWCNTs showed more cytotoxic effect as compared to PTX and PTX-MWCNTs with PTX-Rf-MWCNTs exhibiting the maximum cytotoxic potential. CONCLUSION: Thus in final outcome, we concluded that the riboflavin and thiamine conjugated MWCNTs shown great promising potential in the treatment of cancer, but more exhaustive data is needed in future.


Assuntos
Nanotubos de Carbono/química , Paclitaxel/química , Paclitaxel/farmacologia , Riboflavina/química , Riboflavina/farmacologia , Tiamina/química , Tiamina/farmacologia , Linhagem Celular Tumoral , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Humanos , Células MCF-7
13.
Mol Pharm ; 12(2): 630-43, 2015 Feb 02.
Artigo em Inglês | MEDLINE | ID: mdl-25517904

RESUMO

Our main aim in the present investigation was to assess and compare the in vitro and in vivo cancer targeting propensity of doxorubicin (DOX) loaded folic acid (FA) and estrone (ES) anchored PEGylated multiwalled carbon nanotubes (MWCNTs) employing tumor bearing Balb/c mice. The DOX was loaded into the developed functionalized MWCNTs after proper characterization using dialysis diffusion method. The in vitro, ex vivo, and in vivo studies were performed on the MCF-7 cell line for assessment of the cancer targeting propensity. Both qualitative and quantitative cell uptake studies indicated the preferential higher uptake of estrone anchored nanotube formulation compared to other formulations and free DOX owing to the overexpression of estrogen receptors (ERs) on human breast MCF-7 cells. Similarly, the pharmacokinetic and increased antitumor activities also confirmed the elevated cancer targeting propensity of the estrone and folic acid anchored MWCNT formulations. The DOX/ES-PEG-MWCNTs has also shown significantly longer survival span (43 days) than free DOX (18 days) and control group (12 days). Present outcomes from the ex vivo and in vivo studies are deemed to be of great scientific value and shall assist targeted drug delivery formulation scientists for selection of the targeting moieties in the treatment of human breast cancer.


Assuntos
Doxorrubicina/farmacocinética , Estrona/química , Ácido Fólico/química , Nanotubos de Carbono/química , Animais , Antibióticos Antineoplásicos/administração & dosagem , Antibióticos Antineoplásicos/química , Antibióticos Antineoplásicos/farmacocinética , Neoplasias da Mama/metabolismo , Sobrevivência Celular/fisiologia , Doxorrubicina/administração & dosagem , Doxorrubicina/química , Sistemas de Liberação de Medicamentos/métodos , Feminino , Humanos , Células MCF-7 , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Camundongos Endogâmicos BALB C
14.
Drug Dev Ind Pharm ; 41(11): 1888-901, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25738812

RESUMO

OBJECTIVE: Saquinavir (SQV) is a US-FDA approved HIV protease inhibitor (HPI) for HIV cure. The purpose of the present investigation was to develop and characterize the anticancer potential of the SQV-loaded folic acid (FA) conjugated PEGylated and non-PEGylated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) (SQV-Fol-PEG-PLGA and SQV-Fol-PLGA) employing PC-3 (human prostate) and MCF-7 (human breast) cancer cell lines. MATERIALS AND METHODS: Developed NPs were characterized by IR, NMR, DSC, XRD, size, charge and further tested for drug loading and cellular uptake properties. RESULT: The entrapment efficiency was found to be 56 ± 0.60 and 58 ± 0.80 w/v for SQV-Fol-PEG-PLGA and SQV-PLGA NPs, respectively. The obtained results of SQV-Fol-PEG-PLGA showed enhanced cytotoxicity and cellular uptake and were most preferentially taken up by the cancerous cells via folate receptor-mediated endocytosis (RME) mechanism. At 260 µM concentration, SQV-PLGA NPs and SQV-Fol-PEG-PLGA NPs showed 20%, 20% and 23% cell growth inhibition in PC-3 cells, respectively whereas in MCF-7 cells it was 12%, 15% and 14% cell growth inhibition, respectively. CONCLUSIONS: Developed targeted SQV-Fol-PEG-PLGA NPs were superior anticancer potential as compared to non-targeted SQV-PLGA NPs. Thus, these targeted NPs provide another option for anticancer drug delivery scientists.


Assuntos
Antineoplásicos/administração & dosagem , Ácido Fólico/administração & dosagem , Nanopartículas , Saquinavir/administração & dosagem , Antineoplásicos/química , Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Portadores de Fármacos/química , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Endocitose/efeitos dos fármacos , Feminino , Ácido Fólico/química , Ácido Fólico/farmacologia , Humanos , Ácido Láctico/química , Células MCF-7 , Masculino , Tamanho da Partícula , Poliésteres/química , Polietilenoglicóis/química , Ácido Poliglicólico/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Saquinavir/química , Saquinavir/farmacologia
15.
Pharm Res ; 31(2): 322-34, 2014 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-24043294

RESUMO

PURPOSE: To develop, characterize and exploring the sulfasalazine loaded fucoyslated multi walled carbon nanotubes for Kupffer cell targeting for effective management of cytokine-induce liver damage. METHODS: Sulfasalazine was loaded into the fucosylated MWCNTs after subsequential functionalization (carboxylation, acylation and amidation) using dialysis membrane technique. The in vitro, in vivo studies were performed on macrophages J 774 cell line for Kupffer cells targeting for the treatment of cytokine-induced liver damage. RESULTS: The loading of SSZ into SSZ-FUCO-MWCNTs was 87.77 ± 0.11% (n = 3). Sustained release was obtained from SSZ-FUCO-MWCNTs, with 89.12 ± 0.71% of SSZ released into medium at 48th hr. SSZ-FUCO-MWCNTs showed the 9.0 ± 0.23% hemolysis was drastically reduced from 21.62 ± 0.24% SSZMWCNTs 21.62 ± 0.24%. In SRB assay, SSZ-FUCO-MWCNTs showed more cytotoxicity than raw and SSZ-MWCNTs. In cytokine assay, SSZ- FUCO-MWCNTs exhibited significantly higher inhibition of IL-12 p40 secretion. In Western blot assay, SSZ-FUCO-MWCNTs significantly inhibit NF-κB activation. CONCLUSION: The results suggested that the SSZ-FUCO-MWCNTs may be useful nano-carriers for targeted delivery to Kupffer cells in the treatment of cytokine-induced liver damage.


Assuntos
Citocinas/efeitos adversos , Células de Kupffer/efeitos dos fármacos , Hepatopatias/tratamento farmacológico , Nanotubos de Carbono/química , Sulfassalazina/química , Sulfassalazina/farmacologia , Animais , Linhagem Celular , Preparações de Ação Retardada/química , Preparações de Ação Retardada/farmacologia , Humanos , Macrófagos/efeitos dos fármacos , Masculino , Ratos , Ratos Sprague-Dawley
16.
AAPS PharmSciTech ; 15(2): 388-99, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24431104

RESUMO

Liposomes (LIP), nanoparticles (NP), dendrimers (DEN), and carbon nanotubes (CNTs), represent eminent classes of drug delivery devices. A study was carried out herewith by employing docetaxel (DTX) as model drug to assess their comparative drug delivery potentials. Under optimized conditions, highest entrapment of DTX was observed in CNT-based formulation (DTX-CNTs, 74.70 ± 4.9%) followed by nanoparticles (DTX-NP, 62.34 ± 1.5%), liposome (49.2 ± 1.51%), and dendrimers (28.26 ± 1.74%). All the formulations were found to be of nanometric size. In vitro release studies were carried out in PBS (pH 7.0 and 4.0), wherein all the formulations showed biphasic release pattern. Cytotoxicity assay in human cervical cancer SiHa cells inferred lowest IC50 value of 1,235.09 ± 41.93 nM with DTX-CNTs, followed by DTX-DEN, DTX-LIP, DTX-NP with IC50 values of 1,571.22 ± 151.27, 1,653.98 ± 72.89, 1,922.75 ± 75.15 nM, respectively. Plain DTX showed higher hemolytic toxicity of 22.48 ± 0.94%, however loading of DTX inside nanocarriers drastically reduced its hemolytic toxicity (DTX-DEN, 17.22 ± 0.48%; DTX-LIP, 4.13 ± 0.19%; DTX-NP, 6.43 ± 0.44%; DTX-CNTs, 14.87 ± 1.69%).


Assuntos
Dendrímeros , Ácido Láctico/química , Lipossomos , Nanopartículas , Nanotubos de Carbono , Ácido Poliglicólico/química , Linhagem Celular Tumoral , Humanos , Espectroscopia de Ressonância Magnética , Microscopia Eletrônica de Transmissão , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Espectroscopia de Infravermelho com Transformada de Fourier
17.
Biomater Adv ; 162: 213903, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38824828

RESUMO

AIM: The aim of the present review is to shed light on the nanotechnological approaches adopted to overcome the shortcomings associated with the delivery of venom peptides which possess inherent anti-cancer properties. BACKGROUND: Venom peptides although have been reported to demonstrate anti-cancer effects, they suffer from several disadvantages such as in vivo instability, off-target adverse effects, limited drug loading and low bioavailability. This review presents a comprehensive compilation of different classes of nanocarriers while underscoring their advantages, disadvantages and potential to carry such peptide molecules for in vivo delivery. It also discusses various nanotechnological aspects such as methods of fabrication, analytical tools to assess these nanoparticulate formulations, modulation of nanocarrier polymer properties to enhance loading capacity, stability and improve their suitability to carry toxic peptide drugs. CONCLUSION: Nanotechnological approaches bear great potential in delivering venom peptide-based molecules as anticancer agents by enhancing their bioavailability, stability, efficacy as well as offering a spatiotemporal delivery approach. However, the challenges associated with toxicity and biocompatibility of nanocarriers must be duly addressed. PERSPECTIVES: The everlasting quest for new breakthroughs for safer delivery of venom peptides in human subjects is fuelled by unmet clinical needs in the current landscape of chemotherapy. In addition, exhaustive efforts are required in obtaining and purifying the venom peptides followed by designing and optimizing scale up technologies.


Assuntos
Antineoplásicos , Nanotecnologia , Neoplasias , Humanos , Neoplasias/tratamento farmacológico , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/uso terapêutico , Antineoplásicos/química , Nanotecnologia/métodos , Peçonhas/administração & dosagem , Peçonhas/uso terapêutico , Peçonhas/farmacocinética , Peçonhas/química , Peptídeos/administração & dosagem , Peptídeos/química , Sistemas de Liberação de Medicamentos/métodos , Nanopartículas/química , Portadores de Fármacos/química
18.
Nanomedicine (Lond) ; 2024 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-38700294

RESUMO

Aim: To investigate the pemetrexed encapsulated polymeric mixed micelles (PMMs) against breast cancer treatment. Methods: We meticulously optimized the formulation and conducted extensive characterizations, including photon correlation spectroscopy for micellization, advanced analytical techniques and in vitro cell line assessments. Results: The PMM exhibited favorable characteristics, with a spherical morphology, hydrodynamic particle size of 19.58 ± 0.89 nm, polydispersity index of 0.245 ± 0.1, and a surface charge of -9.70 ± 0.61 mV. Encapsulation efficiency and drug payload reached 96.16 ± 0.37% and 4.5 ± 0.32%, respectively. Cytotoxicity analysis indicated superior efficacy of the PMM over the drug solution. Conclusion: The PMM formulation exhibited controlled release of the drug, and demonstrated enhanced cytotoxicity against breast cancer cells, highlighting its therapeutic promise.

19.
Ther Deliv ; 15(4): 279-303, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38374774

RESUMO

Breast cancer (BC) is a heterogeneous disease with various morphological features, clinicopathological conditions and responses to different therapeutic options, which is responsible for high mortality and morbidity in women. The heterogeneity of BC necessitates new strategies for diagnosis and treatment, which is possible only by cautious harmonization of the advanced nanomaterials. Recent developments in vesicular nanocarrier therapy indicate a paradigm shift in breast cancer treatment by providing an integrated approach to address current issues. This review provides a detailed classification of various nanovesicles in the treatment of BC with a special emphasis on recent advances, challenges in translating nanomaterials and future potentials.


Assuntos
Neoplasias da Mama , Nanopartículas , Nanoestruturas , Feminino , Humanos , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Portadores de Fármacos
20.
Drug Discov Today ; 29(3): 103913, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38340952

RESUMO

The pharmaceutical industry is grappling with a pressing crisis in drug development characterized by soaring R&D costs, setbacks in blockbuster drug development due to poor aqueous solubility, and patent-related limitations on newly approved molecules. To combat these challenges, diverse strategies have emerged to enhance the solubility and dissolution rates of Biopharmaceutics Classification System (BCS) II and IV drug molecules. Enter drug nanocrystals, a revolutionary nanotechnology-driven, carrier-free colloidal drug delivery system. This review provides a comprehensive insight into nanocrystal strategies, stabilizer selection criteria, preparation methods, advanced characterization techniques, the evolving nanocrystal technological landscape, current market options, and exciting clinical prospects for reshaping the future of pharmaceuticals.


Assuntos
Nanopartículas , Preparações Farmacêuticas/química , Nanopartículas/química , Sistemas de Liberação de Medicamentos , Biofarmácia , Nanotecnologia , Solubilidade , Disponibilidade Biológica
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA