Development, In Vitro Characterization, Antitumor and Aerosol Performance Evaluation of Respirable Prepared by Self-nanoemulsification Method

AbstractPoor water solubility and low oral bioavailability limit the clinical application of Erlotinib as an anticancer. For this purpose, we encapsulated erlotinib in the solid lipid nanoparticles (SLN) and designed a spray-dried dry powder inhalable (DPI) formulation. Erlotinib-loaded SLNs were prepared using self-nanoemulsifying and characterized for physicochemical properties. Pulmonary deposition of spray-dried DPI formulation was performed using Next Generation Impactor. The particle size and zeta potential of Erlotinib-loaded SLNs were 300 to 800 nm and −18 to −32 mV, respectively. High drug entrapment efficiency in the narrow range of 80–85% was achieved. Cytotoxicity results indicated that cell growth inhibition of free drug and drug loaded nanoparticles is dose- and time-dependent. Inhalable dry powders prepared from drug-loaded SLNs were found to have a fine particle fraction in the range of 6.92±0.99 –11.24±2.4%, mean mass aerodynamic diameter in the range of 4.52±0.1 to 6.67±0.5 µm. The findings revealed that the proposed inhalable dry powder formulation loaded with erlotinib SLN has potential in lung cancer therapy through pulmonary route.

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Diacerein-Loaded Hyaluosomes as a Dual-Function Platform for Osteoarthritis Management via Intra-Articular Injection: In Vitro Characterization and In Vivo Assessment in a Rat Model

Pharmaceutics ◽

10.3390/pharmaceutics13060765 ◽

2021 ◽

Vol 13 (6) ◽

pp. 765

Author(s):

Nouran O. Abdelmageed ◽

Nadia M. Morsi ◽

Rehab N. Shamma

Keyword(s):

Hyaluronic Acid ◽

Cartilage Damage ◽

Entrapment Efficiency ◽

Dual Function ◽

In Vitro Characterization ◽

Drug Entrapment Efficiency ◽

Formulation Parameters ◽

Acid Gel

The application of intra-articular injections in osteoarthritis management has gained great attention lately. In this work, novel intra-articular injectable hyaluronic acid gel-core vesicles (hyaluosomes) loaded with diacerein (DCN), a structural modifying osteoarthritis drug, were developed. A full factorial design was employed to study the effect of different formulation parameters on the drug entrapment efficiency, particle size, and zeta potential. Results showed that the prepared optimized DCN- loaded hyaluosomes were able to achieve high entrapment (90.7%) with a small size (310 nm). The morphology of the optimized hyaluosomes was further examined using TEM, and revealed spherical shaped vesicles with hyaluronic acid in the core. Furthermore, the ability of the prepared DCN-loaded hyaluosomes to improve the in vivo inflammatory condition, and deterioration of cartilage in rats (injected with antigen to induce arthritis) following intra-articular injection was assessed, and revealed superior function on preventing cartilage damage, and inflammation. The inflammatory activity assessed by measuring the rat’s plasma TNF-α and IL-1b levels, revealed significant elevation in the untreated group as compared to the treated groups. The obtained results show that the prepared DCN-loaded hyaluosomes would represent a step forward in the design of novel intra articular injection for management of osteoarthritis.

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Inhalable Spray Dried Pro-Liposome Powder Containing Budesonide for Pulmonary Delivery

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2021.14.4.3 ◽

2021 ◽

Vol 14 (4) ◽

pp. 5538-5548

Author(s):

Aliasgar J Kundawala ◽

Khushbu S Chauhan ◽

Harsha V Patel ◽

Swati K Kurtkoti

Keyword(s):

Drug Release ◽

Spray Drying ◽

Entrapment Efficiency ◽

Geometric Standard Deviation ◽

Drying Method ◽

Dry Powder ◽

Liposomal Drug ◽

Vesicle Size ◽

Aerodynamic Properties ◽

Spray Dried

Budesonide is an anti-asthmatic agent which is used to control the symptoms of asthma like bronchospasm, oedema. Drug delivered to lung through inhalation will provide systemic and local drug delivery at lower dose in chronic and acute diseases. Dry powder inhalers are the best choice for targeting the anti-asthmatic drugs through pulmonary route. The objective of the present study is to prepare inhalable lipid coated budesonide microparticles by spray drying method so effective delivery of budesonide to the lungs can be achieved. The microparticles in the form of dry powder were obtained by either spray drying liposomal drug suspension or lipid drug suspension. The liposomes were initially prepared by solvent evaporation method using Hydrogenated Soyabean Phosphatidylcholine and Cholesterol (1:1, 1:2, 2:1) as lipid carrier and then spray dried later with mannitol as bulking agent at different lipid to diluent ratio (1:1.25, 1:2.5 & 1:5). The liposomes and liposomal dry powder were evaluated for vesicle size, % entrapment efficiency, in vitro drug release studies, powder characteristics, aerosol performance and stability studies. The liposomes prepared showed vesicle size (2-8 µm), Entrapment efficiency (92.22%) at lipid: drug ratio of (2.5:1) and observed 80.41 % drug release in 24 hrs. Pro-liposomes prepared by spray drying of liposomal drug suspension (LSD1) showed emitted dose, mean mass aerodynamic diameter, geometric standard deviation and fine particle fraction of 99.01%, 3.12 µm, 1.78 and 43.5% along with good powder properties. The spray dried powder was found to be stable at 4 ± 2 °C & 65% ± 5 % RH. The inhalable microparticles containing Budesonide containing lipid dry powder was successfully prepared by spray drying method that showed good aerodynamic properties and stability with mannitol as diluent. The microparticles produced with this novel approach could deliver drug on target via inhalation route and also ease manufacture process at large scale in fewer production steps.

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Formulation, characterization and evaluation of nanoparticles based dry powder insufflation containing terbutaline sulphate and itraconazole for the treatment of asthma

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i1.1859 ◽

2020 ◽

Vol 11 (1) ◽

pp. 567-580

Author(s):

Venugopalaiah Penabaka ◽

Kumar B ◽

Prasad N.B.L

Keyword(s):

Particle Size ◽

Size Distribution ◽

Bronchial Asthma ◽

Spherical Particles ◽

Dry Powder ◽

Terbutaline Sulphate ◽

Release Studies ◽

Physical Mixing ◽

Spray Dried

Many factors affect the pulmonary drug delivery and stability of the nanoparticles an acupuncture consisting of bronchial asthma. Present research envisages on the development of dry powder nanoparticles as insufflation a acupuncture consisting of bronchial asthma (allergy due to Aspergillus fumigatus) using physical mixing and spray drying. Different founding are prepared and characterized with suitable excipients like lactose and trehalose. The particle size distribution of nano milled and spray-dried particles of Terbutaline Sulphate and Itraconazole showed unimodal size distribution. The formulations prepared with trehalose as the carrier showed less Dv90, Dv50 and Dv10 values due to the fineness in the particles of trehalose when compared to lactose. The Dv50 and Dv10 values were in the range of mountains of 0.43-0.89 µm and 0.21–0.49 µm for all formulations, which shows the primary particle size in the nanometer scale. Smooth and nearly spherical particles were produced for spray-dried formulations when compared to milled formulations. Zeta potential comes across until be between +17±0.13 to +32±0.12, which explains the particles as moderately stable. MMAD values ranges from 3.19 µm to 4.78 µm for milled nanoparticles and 3.45 µm to 4.21 µm for spray-dried particles. Formulated nanoparticles exhibited good spreading properties, which will allow all the particles to deposition palmy profusion territories consisting of the lung. In-vitro drug release studies explains that spray-dried formulations of Terbutaline sulpahte and Itraconazole using lactose as excipients released the drug upto 98.9% and 99.1% in 180mts.

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Corrigendum to: Transethosomes of Econazole Nitrate for Transdermal Delivery: Development, In-vitro Characterization, and Ex-vivo Assessment

Pharmaceutical Nanotechnology ◽

10.2174/221173850903210813100519 ◽

2021 ◽

Vol 9 (3) ◽

pp. 245-245

Author(s):

Shivani Verma ◽

Puneet Utreja

Keyword(s):

Transdermal Delivery ◽

Ex Vivo ◽

In Vitro Characterization ◽

Research Scholar ◽

Development In Vitro ◽

Econazole Nitrate

The authors wish to add words “Research Scholar” and “Research Supervisor” to their affiliations [1]. The original article can be found online at https://doi.org/10.2174/2211738506666180813122102

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Development of an Innovative, Carrier-Based Dry Powder Inhalation Formulation Containing Spray-Dried Meloxicam Potassium to Improve the In Vitro and In Silico Aerodynamic Properties

Pharmaceutics ◽

10.3390/pharmaceutics12060535 ◽

2020 ◽

Vol 12 (6) ◽

pp. 535 ◽

Cited By ~ 1

Author(s):

Edit Benke ◽

Árpád Farkas ◽

Piroska Szabó-Révész ◽

Rita Ambrus

Keyword(s):

In Silico ◽

Chronic Obstructive ◽

Dry Powder Inhalation ◽

Dry Powder ◽

Aerodynamic Properties ◽

Drug Concentrations ◽

Anti Inflammatory ◽

New Formulation ◽

Spray Dried

Most of the marketed dry powder inhalation (DPI) products are traditional, carrier-based formulations with low drug concentrations deposited in the lung. However, due to their advantageous properties, their development has become justified. In our present work, we developed an innovative, carrier-based DPI system, which is an interactive physical blend of a surface-modified carrier and a spray-dried drug with suitable shape and size for pulmonary application. Meloxicam potassium, a nonsteroidal anti-inflammatory drug (NSAID), was used as an active ingredient due to its local anti-inflammatory effect and ability to decrease the progression of cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). The results of the in vitro and in silico investigations showed high lung deposition in the case of this new formulation, confirming that the interparticle interactions were changed favorably.

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Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study

Pharmaceutics ◽

10.3390/pharmaceutics12050465 ◽

2020 ◽

Vol 12 (5) ◽

pp. 465 ◽

Cited By ~ 4

Author(s):

Eman A. Mazyed ◽

Abdelaziz E. Abdelaziz

Keyword(s):

Ex Vivo ◽

Entrapment Efficiency ◽

Tween 80 ◽

Ocular Delivery ◽

Ethanol Injection ◽

In Vitro Characterization ◽

Span 60 ◽

In Vivo Characterization

Acetazolamide (ACZ) is a potent carbonic anhydrase inhibitor that is used for the treatment of glaucoma. Its oral administration causes various undesirable side effects. This study aimed to formulate transgelosomes (TGS) for enhancing the ocular delivery of ACZ. ACZ-loaded transfersomes were formulated by the ethanol injection method, using phosphatidylcholine (PC) and different edge activators, including Tween 80, Span 60, and Cremophor RH 40. The effects of the ratio of lipid to surfactant and type of surfactant on % drug released after 8 h (Q8h) and entrapment efficiency (EE%) were investigated by using Design-Expert software. The optimized formula was formulated as TGS, using poloxamers as gelling agents. In vitro and in vivo characterization of ACZ-loaded TGS was performed. According to optimization study, F8 had the highest desirability value and was chosen as the optimized formula for preparing TGS. F8 appeared as spherical elastic nanovesicles with Q8h of 93.01 ± 3.76% and EE% of 84.44 ± 2.82. Compared to a free drug, TGS exhibited more prolonged drug release of 71.28 ± 0.46% after 8 h, higher ex vivo permeation of 66.82 ± 1.11% after 8 h and a significant lowering of intraocular pressure (IOP) for 24 h. Therefore, TGS provided a promising technique for improving the corneal delivery of ACZ.

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Preparation and in vitro characterization of valsartan-loaded ethyl cellulose and poly(methyl methacrylate) nanoparticles

RSC Advances ◽

10.1039/d0ra07218d ◽

2020 ◽

Vol 10 (72) ◽

pp. 43915-43926

Author(s):

Eszter Hajba-Horváth ◽

Emese Biró ◽

Mirella Mirankó ◽

Andrea Fodor-Kardos ◽

László Trif ◽

...

Keyword(s):

Methyl Methacrylate ◽

Intestinal Absorption ◽

Ethyl Cellulose ◽

Active Agent ◽

Poly Methyl Methacrylate ◽

In Vitro Characterization ◽

Spray Dried

Valsartan-loaded ethyl cellulose and poly(methyl methacrylate) nanoparticles were prepared and nano spray-dried. The active agent was structurally changed in the nanoparticles, which could be advantageous in the intestinal absorption.

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