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Article ; Online: Lipid-nucleic acid nanoparticles of novel ionizable lipids for systemic BMP-9 gene delivery to bone-marrow mesenchymal stem cells for osteoinduction.

Vhora, Imran / Lalani, Rohan / Bhatt, Priyanka / Patil, Sushilkumar / Misra, Ambikanandan

2019 Volume 563, Page(s) 324–336

Abstract: Rational design of novel ionizable lipids for development of lipid-nucleic acid nanoparticles (LNP) is required for safe and effective systemic gene delivery for osteoporosis. LNPs require suitable characteristics for intravenous administration and ... ...

Abstract	Rational design of novel ionizable lipids for development of lipid-nucleic acid nanoparticles (LNP) is required for safe and effective systemic gene delivery for osteoporosis. LNPs require suitable characteristics for intravenous administration and effective accumulation in bone marrow for enhanced transfection. Hence, lipids with C18 tail and ionizable headgroup (Boc-His-ODA/BHODA and His-ODA/HODA) were synthesized and characterized physicochemically. LNPs were prepared with bone morphogenetic protein-9 gene (BHODA-LNP, HODA-LNP, and bone-homing peptide targeted HODA-LNP - HODA-LNPT). Thorough physicochemical (electrolyte stability, DNase I and serum stability) and biological (hemolysis, ROS induction, cytotoxicity and transfection) characterization was carried out followed by acute toxicity studies and therapeutic performance studies in ovariectomized rat model. Lipids with pH dependent ionization were successfully synthesized. LNPs thereof were ∼100 nm size with stability against electrolytes, DNase I and serum and exhibited low hemolytic potential demonstrating suitability for intravenous administration. LNPs exhibited minimal cytotoxicity, non-significant ROS induction and high transfection. In vivo studies demonstrated safety and improved bone regeneration in OVX rats with HODA-LNPT showing significantly better performance. Synthesized ionizable lipids offer safe and effective alternative for preparation of LNPs for gene delivery. Targeted BMP-9 LNP show potential for systemic osteoporosis treatment.
MeSH term(s)	Animals ; Bone Marrow Cells/cytology ; Cell Line ; DNA/administration & dosage ; Erythrocytes/physiology ; Female ; Gene Transfer Techniques ; Growth Differentiation Factors/genetics ; Lipids/administration & dosage ; Mesenchymal Stem Cells/metabolism ; Mice ; Nanoparticles/administration & dosage ; Osteogenesis ; Osteoporosis/therapy ; Ovariectomy ; Plasmids ; Rats, Sprague-Dawley ; Reactive Oxygen Species/metabolism
Chemical Substances	Growth Differentiation Factors ; Lipids ; Reactive Oxygen Species ; DNA (9007-49-2)
Language	English
Publishing date	2019-04-05
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2019.04.006
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Zs.A 1409: Show issues

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Article ; Online: Co-delivery of cisplatin and siRNA through hybrid nanocarrier platform for masking resistance to chemotherapy in lung cancer.

Patel, Vivek / Lalani, Rohan / Vhora, Imran / Bardoliwala, Denish / Patel, Akanksha / Ghosh, Saikat / Misra, Ambikanandan

Drug delivery and translational research

2020 Volume 11, Issue 5, Page(s) 2052–2071

Abstract: The resistance of cancer cells to chemotherapy has presented a formidable challenge. The current research aims at evaluating whether silencing of the cisplatin efflux promoter gene ABCC3 using siRNA co-loaded with the drug in a nanocarrier improves its ... ...

Abstract	The resistance of cancer cells to chemotherapy has presented a formidable challenge. The current research aims at evaluating whether silencing of the cisplatin efflux promoter gene ABCC3 using siRNA co-loaded with the drug in a nanocarrier improves its efficacy in non-small cell lung cancer (NSCLC). Hybrid nanocarriers (HNCs) comprising lipids and poly(lactic acid-polyethylene glycol) di-block copolymer (PEG-PLA) were prepared for achieving the simultaneous delivery of cisplatin caprylate and ABCC3-siRNA to the cancer cells. PEGylation of the formulated HNCs was carried out using post-insertion technique for imparting long circulation characteristics to the carrier. The optimized formulation exhibited an entrapment efficiency of 71.9 ± 2.2% and 95.83 ± 0.39% for cisplatin caprylate and siRNA respectively. Further, the HNC was found to have hydrodynamic diameter of 153.2 ± 1.76 nm and + 25.39 ± 0.49 mV zeta potential. Morphological evaluation using cryo transmission electron microscopy confirmed the presence of lipid bilayer surrounding the polymeric core in HNCs. The in vitro cellular uptake studies showed improved uptake, while cell viability studies of the co-loaded formulation in A549 cell-line indicated significantly improved cytotoxic potential when compared with drug solution and drug-loaded HNCs; cell cycle analysis indicated increased percentage of cell arrest in G2-M phase compared with drug-loaded HNCs. Further, the gene knock-down study showed that silencing of ABCC3 mRNA might be improved in vitro efficacy of the formulation. The optimized cisplatin and ABCC3 siRNA co-loaded formulation presented significantly increased half-life and tumour regression in A549 xenograft model in BALB/c nude mice. In conclusion, siRNA co-loaded formulation presented reduced drug resistance and increased efficacy, which might be promising for the current cisplatin-based treatments in NSCLC.
MeSH term(s)	Animals ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Carcinoma, Non-Small-Cell Lung/metabolism ; Cell Line, Tumor ; Cisplatin/pharmacology ; Cisplatin/therapeutic use ; Humans ; Lung Neoplasms/genetics ; Mice ; Mice, Nude ; Nanoparticles ; Polyethylene Glycols/therapeutic use ; RNA, Small Interfering
Chemical Substances	RNA, Small Interfering ; Polyethylene Glycols (3WJQ0SDW1A) ; Cisplatin (Q20Q21Q62J)
Language	English
Publishing date	2020-11-11
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2590155-2
ISSN	2190-3948 ; 2190-393X
ISSN (online)	2190-3948
ISSN	2190-393X
DOI	10.1007/s13346-020-00867-5
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Article ; Online: Hydroxyethyl substituted linear polyethylenimine for safe and efficient delivery of siRNA therapeutics.

Patil, Sushilkumar / Lalani, Rohan / Bhatt, Priyanka / Vhora, Imran / Patel, Vivek / Patel, Hinal / Misra, Ambikanandan

RSC advances

2018 Volume 8, Issue 62, Page(s) 35461–35473

Abstract: Linear polyethylenimine (LPEI) has been well reported as a carrier for siRNA delivery. However, its applications are limited due to its highly ionized state at physiologic pH and the resultant charge mediated toxicity. The presence of ionizable secondary ...

Abstract	Linear polyethylenimine (LPEI) has been well reported as a carrier for siRNA delivery. However, its applications are limited due to its highly ionized state at physiologic pH and the resultant charge mediated toxicity. The presence of ionizable secondary amines in LPE are responsible for its unique characteristics such as pH dependent solubility and positive charge. Therefore, modification of LPEI was carried out to obtain hydroxyethyl substituted LPEI with the degree of substitution ranging from 15% to 45%. The impact of modification on the physicochemical parameters of the polymer,
Language	English
Publishing date	2018-10-16
Publishing country	England
Document type	Journal Article
ISSN	2046-2069
ISSN (online)	2046-2069
DOI	10.1039/c8ra06298f
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Article: Protein- and Peptide-drug conjugates: an emerging drug delivery technology.

Vhora, Imran / Patil, Sushilkumar / Bhatt, Priyanka / Misra, Ambikanandan

Advances in protein chemistry and structural biology

2015 Volume 98, Page(s) 1–55

Abstract: Protein- and peptide-drug conjugates hold a promising stance in the delivery of therapeutic agents by providing distinct advantage of improving therapeutic potential of drugs. Recent advancements in the proteomics and recombinant DNA technology, by ... ...

Abstract	Protein- and peptide-drug conjugates hold a promising stance in the delivery of therapeutic agents by providing distinct advantage of improving therapeutic potential of drugs. Recent advancements in the proteomics and recombinant DNA technology, by enabling identification of distinct structural features of proteins and making it feasible to introduce specific functionalities in protein/peptide structure, has made it possible to synthesize high quality protein- and peptide-drug conjugates though a wide variety of coupling techniques. Additionally, use of specialized linkers makes them unique in their in vivo therapeutic application by providing target tissue-specific release of drug. Several protein- and peptide-drug conjugates are currently under clinical trials warranting their huge market potential in near future. Increased understanding in this field will surely enable us to produce high quality protein- and peptide-drug conjugates which will serve therapeutic needs demanded from drug delivery systems in clinical settings.
MeSH term(s)	Albumins/chemistry ; Antibodies/chemistry ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell-Penetrating Peptides/chemistry ; Delayed-Action Preparations/chemistry ; Drug Carriers/chemistry ; Gelatin/chemistry ; Humans ; Immunoconjugates/chemistry ; Molecular Targeted Therapy/methods ; Neoplasms/drug therapy ; Oligopeptides/chemistry ; RNA, Small Interfering/chemistry ; Transferrin/chemistry
Chemical Substances	Albumins ; Antibodies ; Antineoplastic Agents ; Cell-Penetrating Peptides ; Delayed-Action Preparations ; Drug Carriers ; Immunoconjugates ; Oligopeptides ; RNA, Small Interfering ; Transferrin ; arginyl-glycyl-aspartic acid (78VO7F77PN) ; Gelatin (9000-70-8)
Language	English
Publishing date	2015
Publishing country	Netherlands
Document type	Journal Article ; Review
ISSN	1876-1623
ISSN	1876-1623
DOI	10.1016/bs.apcsb.2014.11.001
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Article ; Online: Liposomes and Lipid Envelope-Type Systems for Systemic siRNA Delivery.

Vhora, Imran / Patil, Sushilkumar / Amrutiya, Jitendra / Misra, Ambikanandan

Current pharmaceutical design

2015 Volume 21, Issue 31, Page(s) 4541–4555

Abstract: The 'RNA interference' has emerged as a potential therapeutic strategy owing to its high specificity to silent any malfunctioned gene in diseases with genetic background. Currently intravenous delivery of siRNA has been a preferred way of administration ... ...

Abstract	The 'RNA interference' has emerged as a potential therapeutic strategy owing to its high specificity to silent any malfunctioned gene in diseases with genetic background. Currently intravenous delivery of siRNA has been a preferred way of administration due to high access of blood to the organs where direct delivery is not possible. Among non-viral delivery systems enabling systemic delivery of siRNA, liposomes and lipid envelope systems appear to be promising due to their biocompatibility over other systems. However, these systems are still challenged by toxicity issues, instability in blood, non-specific distribution and low transfection efficiency after intravenous administration. Therefore, to increase the success of lipid based siRNA delivery, it is essential to understand the importance of various factors affecting the efficiency of siRNA delivery. The current review focuses on the formulation of lipid based siRNA formulations, the challenges posed in systemic delivery and various aspects affecting the transfection efficiency of such formulations. The review also focuses on emerging strategies for lipid based siRNA delivery and overviews clinical prospects for better development of siRNA delivery systems in future. Considering the current trends, it seems that liposomes and lipid based envelope systems for systemic delivery of siRNA will translate into extensive clinical application overcoming the associated challenges in near future.
MeSH term(s)	Animals ; Gene Transfer Techniques ; Genetic Therapy/methods ; Humans ; Lipids/chemistry ; Liposomes ; RNA Interference ; RNA, Small Interfering/administration & dosage ; Transfection
Chemical Substances	Lipids ; Liposomes ; RNA, Small Interfering
Language	English
Publishing date	2015-08-25
Publishing country	United Arab Emirates
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	1304236-1
ISSN	1873-4286 ; 1381-6128
ISSN (online)	1873-4286
ISSN	1381-6128
DOI	10.2174/138161282131151013185850
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Zs.A 4714: Show issues

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Article ; Online: Colloidally Stable Small Unilamellar Stearyl Amine Lipoplexes for Effective BMP-9 Gene Delivery to Stem Cells for Osteogenic Differentiation.

Vhora, Imran / Lalani, Rohan / Bhatt, Priyanka / Patil, Sushilkumar / Patel, Hinal / Patel, Vivek / Misra, Ambikanandan

AAPS PharmSciTech

2018 Volume 19, Issue 8, Page(s) 3550–3560

Abstract: The biocompatibility of cationic liposomes has led to their clinical translation in gene delivery and their application apart from cancer to cardiovascular diseases, osteoporosis, metabolic diseases, and more. We have prepared PEGylated stearyl amine ( ... ...

Abstract	The biocompatibility of cationic liposomes has led to their clinical translation in gene delivery and their application apart from cancer to cardiovascular diseases, osteoporosis, metabolic diseases, and more. We have prepared PEGylated stearyl amine (pegSA) lipoplexes meticulously considering the physicochemical properties and formulation parameters to prepare single unilamellar vesicles (SUV) of < 100 nm size which retain their SUV nature upon complexation with pDNA rather than the conventional lipoplexes which show multilamellar nature. The developed PEGylated SA lipoplexes (pegSA lipoplexes) showed a lower N/P ratio (1.5) for BMP-9 gene complexation while maintaining the SUV character with a unique shape (square and triangular lipoplexes). Colloidal and pDNA complexation stability in the presence of electrolytes and serum indicates the suitability for intravenous administration for delivery of lipoplexes to bone marrow mesenchymal stem cells through sinusoidal vessels in bone marrow. Moreover, lower charge density of lipoplexes and low oxidative stress led to lower toxicity of lipoplexes to the C2C12 cells, NIH 3T3 cells, and erythrocytes. Transfection studies showed efficient gene delivery to C2C12 cells inducing osteogenic differentiation through BMP-9 expression as shown by enhanced calcium deposition in vitro, proving the potential of lipoplexes for bone regeneration. In vivo acute toxicity studies further demonstrated safety of the developed lipoplexes. Developed pegSA lipoplexes show potential for further in vivo preclinical evaluation to establish the proof of concept.
MeSH term(s)	Amines/chemistry ; Animals ; Cell Differentiation ; Colloids/chemistry ; Gene Transfer Techniques ; Growth Differentiation Factor 2/genetics ; Humans ; Liposomes/chemistry ; Mice ; Osteogenesis ; Stem Cells/metabolism
Chemical Substances	Amines ; Colloids ; Growth Differentiation Factor 2 ; Liposomes ; stearylamine (FFV58UNY7O)
Language	English
Publishing date	2018-09-05
Publishing country	United States
Document type	Journal Article
ISSN	1530-9932
ISSN (online)	1530-9932
DOI	10.1208/s12249-018-1161-6
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Article ; Online: Tacrolimus Loaded PEG-Cholecalciferol Based Micelles for Treatment of Ocular Inflammation.

Kutlehria, Shallu / Vhora, Imran / Bagde, Arvind / Chowdhury, Nusrat / Behl, Gautam / Patel, Ketan / Singh, Mandip

Pharmaceutical research

2018 Volume 35, Issue 6, Page(s) 117

Abstract: Purpose: Poor corneal permeability, nasolacrimal drainage and requirement of chronic administration are major drawbacks of existing therapies for ocular inflammation. Hence, we designed topical micelles of PEG: Methods: Integrin targeted tacrolimus ... ...

Abstract	Purpose: Poor corneal permeability, nasolacrimal drainage and requirement of chronic administration are major drawbacks of existing therapies for ocular inflammation. Hence, we designed topical micelles of PEG Methods: Integrin targeted tacrolimus loaded PEGCCF micelles (TTM) were prepared by solvent diffusion evaporation method and characterized for particle size, osmolality, encapsulation efficiency and drug loading. Therapeutic potential of TTM was evaluated in benzalkonium chloride induced ocular inflammation model in BALB/c mice. Corneal flourescein staining and histopathological analysis of corneal sections was performed. Results: TTM had a particle size of 45.3 ± 5.3 nm, encapsulation efficiency (88.7 ± 0.9%w/w) and osmolality of 292-296 mOsmol/Kg. TTM significantly reduced the corneal fluorescence as compared to tacrolimus suspension (TACS). H&E staining showed that TTM could restore corneal epithelial thickness, reduce stromal edema (p < 0.05) and decrease number of inflammatory cells (p < 0.01) compared with TACS. Immunohistochemistry analysis demonstrated lower expression of Ki67 + ve cells (p < 0.05) and IL-6 throughout the cornea against TACS (p < 0.01) and the control (p < 0.001). Conclusions: TTM is an innovative delivery system for improving ocular inflammation due to a) integrin targeting b) PEGCCF in the form of carrier and c) anti-inflammatory and synergistic effect (due to Pgp inhibition) with TAC.
MeSH term(s)	Administration, Ophthalmic ; Animals ; Benzalkonium Compounds/toxicity ; Cholecalciferol/chemistry ; Disease Models, Animal ; Drug Carriers/chemistry ; Drug Compounding/methods ; Eye/drug effects ; Eye/pathology ; Eye Diseases/chemically induced ; Eye Diseases/drug therapy ; Eye Diseases/pathology ; Female ; Humans ; Inflammation/chemically induced ; Inflammation/drug therapy ; Inflammation/pathology ; Integrins/metabolism ; Mice ; Mice, Inbred BALB C ; Micelles ; Polyethylene Glycols/chemistry ; Tacrolimus/administration & dosage ; Tacrolimus/pharmacokinetics
Chemical Substances	Benzalkonium Compounds ; Cholecalciferol-PEG Conjugate ; Drug Carriers ; Integrins ; Micelles ; Cholecalciferol (1C6V77QF41) ; Polyethylene Glycols (3WJQ0SDW1A) ; Tacrolimus (WM0HAQ4WNM)
Language	English
Publishing date	2018-04-16
Publishing country	United States
Document type	Journal Article
ZDB-ID	843063-9
ISSN	1573-904X ; 0724-8741 ; 0739-0742
ISSN (online)	1573-904X
ISSN	0724-8741 ; 0739-0742
DOI	10.1007/s11095-018-2376-7
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Zs.A 1937: Show issues

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Article ; Online: Development of Hot Melt Extruded Solid Dispersion of Tamoxifen Citrate and Resveratrol for Synergistic Effects on Breast Cancer Cells.

Chowdhury, Nusrat / Vhora, Imran / Patel, Ketan / Bagde, Arvind / Kutlehria, Shallu / Singh, Mandip

AAPS PharmSciTech

2018 Volume 19, Issue 7, Page(s) 3287–3297

Abstract: Primary standard therapy for ER-positive breast cancer being tamoxifen, newer delivery approach for enhancement of dissolution and therapeutic efficiency of tamoxifen through oral route could be a possible solution. In the present study, we investigated ... ...

Abstract	Primary standard therapy for ER-positive breast cancer being tamoxifen, newer delivery approach for enhancement of dissolution and therapeutic efficiency of tamoxifen through oral route could be a possible solution. In the present study, we investigated combination of tamoxifen (TAM) with resveratrol (RES) and observed that the combination is effective on MCF-7 breast cancer cells. To ensure co-delivery of the drugs, we explored the hot melt extrusion technique for simultaneously extruding two drugs together in order to enhance their bioavailability. As both are class II drugs with dissolution limited bioavailability, detailed formulation and process parameter analyses were carried out. Detailed characterization using microscopy, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD) confirmed that both the drugs were molecularly dispersed in the matrix of Soluplus, CremophorRH40, and Poloxamer188, and no interactions between the ingredients were there during hot melt extrusion (HME) process. Dissolution studies confirmed that HME extrudates were able to release drug more rapidly than simple suspension formulation. Further, pharmacokinetic studies in rats were carried out for tamoxifen. Results demonstrated that extrusion significantly increased the tamoxifen oral bioavailability (p < 0.05) (T
MeSH term(s)	Administration, Oral ; Animals ; Antineoplastic Agents, Hormonal/administration & dosage ; Antineoplastic Agents, Hormonal/chemistry ; Antineoplastic Agents, Hormonal/metabolism ; Antineoplastic Agents, Phytogenic/administration & dosage ; Antineoplastic Agents, Phytogenic/chemistry ; Antineoplastic Agents, Phytogenic/metabolism ; Antineoplastic Combined Chemotherapy Protocols/administration & dosage ; Antineoplastic Combined Chemotherapy Protocols/chemistry ; Antineoplastic Combined Chemotherapy Protocols/metabolism ; Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; Calorimetry, Differential Scanning/methods ; Chemistry, Pharmaceutical/methods ; Drug Development/methods ; Drug Synergism ; Hot Temperature ; Humans ; MCF-7 Cells ; Rats ; Rats, Sprague-Dawley ; Resveratrol/administration & dosage ; Resveratrol/chemistry ; Resveratrol/metabolism ; Spectroscopy, Fourier Transform Infrared/methods ; Tamoxifen/administration & dosage ; Tamoxifen/chemistry ; Tamoxifen/metabolism ; X-Ray Diffraction/methods
Chemical Substances	Antineoplastic Agents, Hormonal ; Antineoplastic Agents, Phytogenic ; Tamoxifen (094ZI81Y45) ; Resveratrol (Q369O8926L)
Language	English
Publishing date	2018-09-14
Publishing country	United States
Document type	Journal Article
ZDB-ID	2052070-0
ISSN	1530-9932 ; 1530-9932
ISSN (online)	1530-9932
ISSN	1530-9932
DOI	10.1208/s12249-018-1111-3
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Article ; Online: Surface-modified Epirubicin-HCl liposomes and its in vitro assessment in breast cancer cell-line: MCF-7.

Gandhi, Ravi / Khatri, Nirav / Baradia, Dipesh / Vhora, Imran / Misra, Ambikanandan

Drug delivery

2016 Volume 23, Issue 4, Page(s) 1152–1162

Abstract: Background: Epirubicin-HCl is highly efficient for breast cancer management at a concentration of 60-90 mg/m(2). However, its application is limited due to cumulative dose-dependent cardio-toxicity.: Purpose: The main aim of this study was to ... ...

Abstract	Background: Epirubicin-HCl is highly efficient for breast cancer management at a concentration of 60-90 mg/m(2). However, its application is limited due to cumulative dose-dependent cardio-toxicity. Purpose: The main aim of this study was to formulate breast cancer-targeted liposomal carrier by surface conjugation of transferrin to minimize cardio-toxicity of drug along with improved pharmacokinetic profile. Method: Liposomes were formulated by ethanol injection method using HSPC, cholesterol and DSPG and later loaded with drug by the ammonium sulfate gradient method. The formulation was characterized for physicochemical properties like size, zeta potential, entrapment efficiency, TEM; in vitro tests like electro-flocculation, hemolysis and drug release; cell line study (MCF-7 cells); in vivo studies including LD50 determination, pharmacokinetic analysis, myocardial toxicity determination and stability. Results and discussion: Optimized formulation had molar ratio of 60:30:8:2 (HSPC:Chol:DSPG:mPEG-DSPE) with entrapment efficiency ∼83%, particle size below 200 nm and zeta potential about -20 mV. In vitro studies proved non-interfering property and drug release character of formulation while cell line studies demonstrated improvement in cell uptake and thereby increased cytotoxicity of targeted formulation. The IC50 value obtained for epirubicin solution, non-targeted and targeted liposomes was 0.675, 0.532 and 0.192 µg/ml, respectively. Furthermore, in vivo tests validated safety and distribution profile of prepared formulations. Conclusion: Apt properties of prepared Epirubicin-HCl liposomal formulation warrant its clinical application in breast cancer treatment after further studies.
MeSH term(s)	Breast Neoplasms/chemistry ; Breast Neoplasms/physiopathology ; Cell Line, Tumor ; Cholesterol/chemistry ; Drug Delivery Systems ; Drug Liberation ; Epirubicin/chemistry ; Epirubicin/pharmacokinetics ; Female ; Humans ; Lipids/chemistry ; Lipids/pharmacokinetics ; Liposomes ; MCF-7 Cells ; Particle Size ; Polyethylene Glycols/administration & dosage ; Polyethylene Glycols/chemistry ; Transferrin/chemistry ; Transferrin/pharmacokinetics
Chemical Substances	Lipids ; Liposomes ; Transferrin ; Polyethylene Glycols (30IQX730WE) ; Epirubicin (3Z8479ZZ5X) ; Cholesterol (97C5T2UQ7J)
Language	English
Publishing date	2016-05
Publishing country	England
Document type	Journal Article
ZDB-ID	1213261-5
ISSN	1521-0464 ; 1071-7544
ISSN (online)	1521-0464
ISSN	1071-7544
DOI	10.3109/10717544.2014.999960
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Zs.A 4252: Show issues

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Article ; Online: Liposomes encapsulating native and cyclodextrin enclosed paclitaxel: Enhanced loading efficiency and its pharmacokinetic evaluation.

Bhatt, Priyanka / Lalani, Rohan / Vhora, Imran / Patil, Sushilkumar / Amrutiya, Jitendra / Misra, Ambikanandan / Mashru, Rajashree

International journal of pharmaceutics

2017 Volume 536, Issue 1, Page(s) 95–107

Abstract: Combination strategy involving cyclodextrin (CD) complexation and liposomal system was investigated for Paclitaxel (PTX) to improve loading. Complexation was done using 2,6-di-O-methylbetacyclodextrin (DMβCD). Sterically stabilized double loaded ... ...

Abstract	Combination strategy involving cyclodextrin (CD) complexation and liposomal system was investigated for Paclitaxel (PTX) to improve loading. Complexation was done using 2,6-di-O-methylbetacyclodextrin (DMβCD). Sterically stabilized double loaded PEGylated liposomes (DLPLs) containing PTX and PTX-DMβCD complex were prepared by thin film hydration. Physicochemical characterization of complex and prepared DLPLs was carried out. Cytotoxic potential, hemolytic potential and pharmacokinetics of DLPLs were tested in comparison to Taxol
MeSH term(s)	Angiogenesis Inhibitors/chemistry ; Angiogenesis Inhibitors/pharmacokinetics ; Animals ; Antineoplastic Agents, Phytogenic/chemistry ; Antineoplastic Agents, Phytogenic/pharmacokinetics ; Cell Line, Tumor ; Cyclodextrins/chemistry ; Drug Carriers/chemistry ; Female ; Humans ; Liposomes/chemistry ; Mice ; Mice, Inbred BALB C ; Paclitaxel/chemistry ; Paclitaxel/pharmacokinetics ; Particle Size ; Rats ; Rats, Sprague-Dawley
Chemical Substances	Angiogenesis Inhibitors ; Antineoplastic Agents, Phytogenic ; Cyclodextrins ; Drug Carriers ; Liposomes ; Paclitaxel (P88XT4IS4D)
Language	English
Publishing date	2017-11-22
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2017.11.048
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