scholarly journals Novel Nanoparticle Biomaterial of Alginate/Chitosan Loading Simultaneously Lovastatin and Ginsenoside RB1: Characteristics, Morphology, and Drug Release Study

2021 ◽  
Vol 2021 ◽  
pp. 1-14
Author(s):  
Quan Vo-An ◽  
Thuy Chinh Nguyen ◽  
Quang Tung Nguyen ◽  
Quoc Trung Vu ◽  
Cong Doanh Truong ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Tripolyphosphate ◽  
Poorly Soluble Drugs ◽  
Drug Solubility ◽  
Ginsenoside Rb1 ◽  
Scanning Calorimetry ◽  
Release Process ◽  
Polymeric Particles ◽  
Poorly Soluble ◽  
Initial Content

Recently, plenty of interesting studies on improvement of bioavailability for poorly soluble drugs were implemented with different approaches such as using of combined biopolymers as a delivery system that allowed to enhancing drug solubility and bioavailability. In this work, alginate and chitosan were blended together in the form of polymeric particles, loaded with both lovastatin and ginsenoside Rb1 to producing the four-component nanoparticles by ionic gelation method. CaCl2 and sodium tripolyphosphate were used as gelation agent and cross-linking agent, respectively. The characteristics of obtained nanoparticles were studied by means of infrared spectra (IR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and dynamic light scattering (DLS). In combination, ginsenoside Rb1 and lovastatin both interacted with each other to improve the drug release ability of the polymer particles. The change of initial content of drugs in the nanoparticles has a negligible effect on the functional groups in the structure of the nanoparticles but has a significant impact on drug release process of both lovastatin and ginsenoside Rb1 from the nanoparticles in selective simulated body fluids. In addition, the synergistic interaction of lovastatin and ginsenoside Rb1 could be also observed through the modification of relative crystal degree and drug release efficiency.

scholarly journals Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

2019 ◽  
Vol 28 (2) ◽  
pp. 105-114
Author(s):  
Samer K. Ali ◽  
Eman B. H. Al-Khedairy
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Drug Solubility ◽  
Scanning Calorimetry ◽  
Poorly Soluble

            Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.           The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents.            All solid dispersion adsorbate (SDA) formulas  were prepared in ratios of 1:1:1  (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content,  , dissolution, crystal structure using  X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC)  studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction.                The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38  fold increase in solubility compared to  solubility of pure ATR and  solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility  and  dissolution .

scholarly journals Low-Surfactant Microemulsions for Enhanced Topical Delivery of Poorly Soluble Drugs

2011 ◽  
Vol 14 (3) ◽  
pp. 315 ◽  
Author(s):  
Alireza Shalviri ◽  
Avinash C Sharma ◽  
Dipak Patel ◽  
Amyn Sayani
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Colloidal Silica ◽  
Topical Delivery ◽  
Silica Gels ◽  
Poorly Soluble Drugs ◽  
Release Rates ◽  
Significant Difference ◽  
Poorly Soluble ◽  
Model Drug

Purpose: To develop and characterize low-surfactant microemulsion (ME) gels to enhance topical delivery of poorly soluble drugs. Method: Five low surfactant ME formulations were manufactured following the construction of pseudo-ternary phase diagrams. The MEs were screened for their ability to dissolve a poorly soluble new chemical entity (Model Drug X). Various viscosity imparting agents like Carbopol 934, Colloidal Silica, HPMC K100M, Lubrajel NP, and Xanthan Gum were evaluated for the manufacture of these ME gels. Each ME gel was then further evaluated for physical stability, including assessing rheological profiles. In vitro release profiles were also determined and compared to a conventional ointment. Results: Three of the five low surfactant MEs developed (ME1, ME4 and ME5) were capable of dissolving Model Drug X up to 14 fold higher than the conventional ointment formulation. ME1 and ME4 gels comprising Xanthan gum or Carbopol 934 were physically stable, while ME5 gel was stable only with Colloidal Silica. The ME5 gel with Colloidal Silica showed an irreversible increase in its elastic modulus when exposed to high temperature, indicating that the formulation would be less suitable for commercial use. The Xanthan Gum and Colloidal Silica gels yielded significantly higher release rates (8 - 10 fold) compared to a conventional ointment and formulations containing Carbopol 934. The significant difference in drug release rates between Xanthan Gum and Carbopol 934 indicated that choice of viscosity imparting agent played an important role in governing drug release from ME gels. Conclusion: ME gels were developed with low surfactant concentrations and improved formulation characteristics, which increased the solubility and subsequent release of a poorly soluble drug. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Novel Poly(L-lactide-co-ε-caprolactone) Matrices Obtained with the Use of Zr[Acac]4as Nontoxic Initiator for Long-Term Release of Immunosuppressive Drugs

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Katarzyna Jelonek ◽  
Janusz Kasperczyk ◽  
Suming Li ◽  
Piotr Dobrzynski ◽  
Henryk Janeczek ◽  
...  
Keyword(s):  
Drug Release ◽  
Cyclosporine A ◽  
Drug Carrier ◽  
Degradation Process ◽  
Lower Amount ◽  
Copolymer Composition ◽  
Scanning Calorimetry ◽  
Release Process ◽  
Copolymer Chain

Slowly degradable copolymers of L-lactide andε-caprolactone can provide long-term delivery and may be interesting as alternative release systems of cyclosporine A (CyA) and rapamycin (sirolimus), in which available dosage forms cause a lot of side effects. The aim of this study was to obtain slowly degradable matrices containing immunosuppressive drug from PLACL initiated by nontoxic Zr[Acac]4. Three kinds of poly(L-lactide-co-ε-caprolactone) (PLACL) matrices with different copolymer chain microstructure were used to compare the release process of cyclosporine A and rapamycine. The influence of copolymer chain microstructure on drug release rate and profile was also analyzed. The determined parameters could be used to tailor drug release by synthesis of demanded polymeric drug carrier. The studied copolymers were characterized at the beginning and during the degradation process of the polymeric matrices by NMR spectroscopy, GPC (gel permeation chromatography), and DSC (differential scanning calorimetry). Different drug release profiles have been observed from each kind of copolymer. The correlation between drug release process and changes of copolymer microstructure during degradation process was noticed. It was determined that different copolymer composition (e.g., lower amount of caprolactone units) does not have to influence the drug release, but even small changes in copolymer randomness affect this process.

scholarly journals SOLUBILITY ENHANCEMENT OF GLIBENCLAMIDE USING MESOPOROUS SILICA

2019 ◽  
pp. 302-314
Author(s):  
Swati Mittal ◽  
AKSHAY SONAWANE ◽  
MANGESH KHUNE
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Drug Loading ◽  
Immediate Release ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Drug Precipitation ◽  
Poorly Soluble

Glibenclamide is a BCS Class II drug and poses a major problem during formulation development. In the present study, adsorption onto various carriers was used to enhance the solubility of glibenclamide. It was observed that solubility of glibenclamide was greatly enhanced by adsorbing onto mesoporous silica. The increase in solubility of poorly soluble drugs is often associated with the generation of supersaturation, which results in the risk of drug precipitation. HPMC E5 was used as precipitation inhibitor to maintain sink condition for a longer duration. A 32 full factorial design was adopted to optimize the ratio of glibenclamide (X1) and mesoporous silica as a carrier (X2) and the effect of different ratios was studied on percent yield, percent drug loading, and percent drug release. X-ray powder diffraction (XRPD) and Differential scanning calorimetry studies were performed to investigate any possible interaction in between glibenclamide and mesoporous silica. An optimum batch of drug adsorbate was used to prepare immediate-release tablets. The tablets prepared were evaluated for thickness, uniformity of weight, hardness, friability, in-vitro disintegration time, and in vitro drug release study.

scholarly journals Formulation and In-Vitro evaluation of Nanocrystal formulation of poorly soluble drugs

2020 ◽  
Vol 9 (4-s) ◽  
pp. 1183-1190
Author(s):  
Arvind Sharma ◽  
Alok Pal Jain ◽  
Sandeep Arora
Keyword(s):  
Particle Size ◽  
In Vitro Study ◽  
Physicochemical Characteristics ◽  
Precipitation Method ◽  
Drug Candidate ◽  
Poorly Soluble Drugs ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Poorly Soluble

Introduction:-Poor solubility of drug compounds which accounts for 40% of new molecules investigated at present is an issue of great concern in pharmaceutical industry and reducing particle size (i,e to reduce below 1000 nm )of drug candidate to be investigated is one of the simplest and efficient ways to overcome this challenge. Drug nanocrystals, solid nanosized drug particles are defined as formulation having 100% drug, which are covered by a stabilizer layer. In this study attempt was made to formulate and evaluate nanocrystals of poorly soluble drugs having low oral bioavailability. Material and method:- Nanocrystals were prepared successfully by varying concentration of different stabilizers by anti-solvent precipitation method. The formulated nanocrystals were evaluated by determining physicochemical characteristics such as physical appearance, Differential Scanning Calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffractometry, solubility studies, particle size distribution, zeta potential, and in vitro drug release profile studies. Results:- An in-vitro study was performed on the successful formulation in comparison to drug powder using dissolution apparatus The particle size of RVT and PSNC-3 was found to be 1975.3 nm and 790.1 nm respectively. Conclusion: Precipitated Nanocrystals formulated with different stablizer’s method resultedin formation of small and uniform RVT nanocrystals with an improved saturation solubility, dissolution rate. Keywords: Nanocrystal, poorly soluble drugs

scholarly journals 3D-Printed Mesoporous Carrier System for Delivery of Poorly Soluble Drugs

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1096
Author(s):  
Christos S. Katsiotis ◽  
Michelle Åhlén ◽  
Maria Strømme ◽  
Ken Welch
Keyword(s):  
Drug Release ◽  
Mesoporous Materials ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Great Promise ◽  
Poorly Soluble Drugs ◽  
Drug Concentrations ◽  
Poorly Soluble ◽  
3D Printed ◽  
Oral Dosage Forms

Fused deposition modelling (FDM) is the most extensively employed 3D-printing technique used in pharmaceutical applications, and offers fast and facile formulation development of personalized dosage forms. In the present study, mesoporous materials were incorporated into a thermoplastic filament produced via hot-melt extrusion and used to produce oral dosage forms via FDM. Mesoporous materials are known to be highly effective for the amorphization and stabilization of poorly soluble drugs, and were therefore studied in order to determine their ability to enhance the drug-release properties in 3D-printed tablets. Celecoxib was selected as the model poorly soluble drug, and was loaded into mesoporous silica (MCM-41) or mesoporous magnesium carbonate. In vitro drug release tests showed that the printed tablets produced up to 3.6 and 1.5 times higher drug concentrations, and up to 4.4 and 1.9 times higher release percentages, compared to the crystalline drug or the corresponding plain drug-loaded mesoporous materials, respectively. This novel approach utilizing drug-loaded mesoporous materials in a printed tablet via FDM shows great promise in achieving personalized oral dosage forms for poorly soluble drugs.

scholarly journals Nanoporous Silica Entrapped Lipid-Drug Complexes for the Solubilization and Absorption Enhancement of Poorly Soluble Drugs

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 63
Author(s):  
Hey-Won Shin ◽  
Joo-Eun Kim ◽  
Young-Joon Park
Keyword(s):  
Ternary Phase Diagram ◽  
Absorption Enhancement ◽  
Nanoporous Silica ◽  
Pharmacokinetic Studies ◽  
Poorly Soluble Drugs ◽  
Scanning Calorimetry ◽  
Significant Difference ◽  
High Dissolution Rate ◽  
Polyethylene Glycol 1000 ◽  
Poorly Soluble

This study aims to examine the contribution of nanoporous silica entrapped lipid-drug complexes (NSCs) in improving the solubility and bioavailability of dutasteride (DUT). An NSC was loaded with DUT (dissolved in lipids) and dispersed at a nanoscale level using an entrapment technique. NSC microemulsion formation was confirmed using a ternary phase diagram, while the presence of DUT and lipid entrapment in NSC was confirmed using scanning electron microscopy. Differential scanning calorimetry and X-ray diffraction revealed the amorphous properties of NSC. The prepared all NSC had excellent flowability and enhanced DUT solubility but showed no significant difference in drug content homogeneity. An increase in the lipid content of NSC led to an increase in the DUT solubility. Further the NSC were formulated as tablets using D-α tocopheryl polyethylene glycol 1000 succinate, glyceryl caprylate/caprate, and Neusilin®. The NSC tablets showed a high dissolution rate of 99.6% at 30 min. Furthermore, NSC stored for 4 weeks at 60 °C was stable during dissolution testing. Pharmacokinetic studies performed in beagle dogs revealed enhanced DUT bioavailability when administered as NSC tablets. NSC can be used as a platform to develop methods to overcome the technical and commercial limitations of lipid-based preparations of poorly soluble drugs.

scholarly journals Ionic Liquid-Polymer Nanoparticle Hybrid Systems as New Tools to Deliver Poorly Soluble Drugs

Nanomaterials ◽  
2019 ◽  
Vol 9 (8) ◽  
pp. 1148 ◽  
Author(s):  
Ana Júlio ◽  
Rita Caparica ◽  
Sofia A. Costa Lima ◽  
Ana Sofia Fernandes ◽  
Catarina Rosado ◽  
...  
Keyword(s):  
Hybrid Systems ◽  
Delivery System ◽  
Freeze Drying ◽  
Poorly Soluble Drugs ◽  
Drug Solubility ◽  
New Paradigm ◽  
Polymer Nanoparticle ◽  
Liquid Polymer ◽  
Cytotoxicity Studies ◽  
Poorly Soluble

The use of functional excipients such as ionic liquids (ILs) and the encapsulation of drugs into nanocarriers are useful strategies to overcome poor drug solubility. The aim of this work was to evaluate the potential of IL-polymer nanoparticle hybrid systems as tools to deliver poorly soluble drugs. These systems were obtained using a methodology previously developed by our group and improved herein to produce IL-polymer nanoparticle hybrid systems. Two different choline-based ILs and poly (lactic-co-glycolic acid) (PLGA) 50:50 or PLGA 75:25 were used to load rutin into the delivery system. The resulting rutin-loaded IL-polymer nanoparticle hybrid systems presented a diameter of 250–300 nm, with a low polydispersity index and a zeta potential of about −40 mV. The drug association efficiency ranged from 51% to 76%, which represents a good achievement considering the poor solubility of rutin. No significant particle aggregation was obtained upon freeze-drying. The presence of the IL in the nanosystem does not affect its sustained release properties, achieving about 85% of rutin released after 72 h. The cytotoxicity studies showed that the delivery system was not toxic to HaCat cells. Our findings may open a new paradigm on the therapy improvement of diseases treated with poorly soluble drugs.

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