Colloidal and vesicular delivery system for herbal bioactive constituents

Pandey, Ravindra Kumar; Bhairam, Monika; Shukla, Shiv Shankar; Gidwani, Bina

doi:10.1007/s40199-021-00403-x

Cited by 29 publications

(9 citation statements)

References 136 publications

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“…A polymer blank solution was made and compared with the sample solution to avoid interference. 5,19,20 The content of DTG (%) in the solid dispersion was calculated according to eq. ( 1) described below:…”

Section: Powder X-ray Diffraction (Pxrd) Studymentioning

confidence: 99%

“…Furthermore, these innovative technologies can control, target, or modulate drug delivery to improve the effect at the action site while reducing unintended and undesirable side effects. 5,6 Dolutegravir (DTG), a recently approved antiviral drug, has solubility concerns because it is a Biopharmaceutical Classification System (BCS) class II candidate. It is an integrase strand transfer inhibitor that prevents the viral DNA from being integrated into the DNA of the host cell, which is thought to be one of the key phases in the life cycle of HIV, and so inhibits the virus from replicating inside the host.…”

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confidence: 99%

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Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Bhairam¹,

Shukla²,

Gidwani³

et al. 2022

IJPQA

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A recently authorized antiviral drug called dolutegravir has solubility problems and could be a Biopharmaceutical Classification System (BCS) class II candidate. The current study aimed to improve dolutegravir’s solubility and efficiency by employing the solid dispersion method. Different ratios of hydrophilic polymeric carriers, including polyethylene glycol (PEG) 6000, polyvinyl pyrrolidone (PVP) (30K), and hydroxypropyl methylcellulose (HPMC), were used. Dolutegravir (DTG) and soluplus were produced as a solid dispersion at 1:5 ratio using the solvent evaporation method. A variety of techniques were utilized to describe the solid state, including powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and fourier transform infrared spectroscopy (FTIR). Produced solid dispersion did not reveal any physicochemical interactions between the DTG and soluplus, but the X-ray diffractogram clearly showed that the drug’s crystalline state had transformed to an amorphous state. DTG was released quickly from solid dispersion (92%) compared to pure drug (10.12%), physical mixture (22.06%), and commercially available DTG (62.90%). The formed solid dispersion’s drug release kinetics was in line with the Higuchi Model. Finally, the rapid drug release from the solid dispersion formulation showed higher Cmax (15.25 ± 0.40 μg/mL) compared to the physical mixture (5.11 ± 0.20 μg/mL) and pure drug (4.91 ± 0.73 μg/mL). DTG’s enhanced bioavailability in experimental wistar rats (AUC: 147.99 ± 23.86 μg/h/mL) further supported this when compared to the AUC of animals administered with physical mixture (52.35 ± 4.32 μg/h/mL) and pure drug (43.32 ± 3.13 μg/h/mL). Thus, it could be inferred that by employing the solid dispersion delivery system and the hydrophilic carrier, soluplus, the bioavailability and dissolution profile of DTG could both be improved, which could be expected to improve the drug’s effectiveness in treating Human immunodeficiency virus/Acquired immunodeficiency syndrome (HIV/AIDS).

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Section: Powder X-ray Diffraction (Pxrd) Studymentioning

confidence: 99%

mentioning

confidence: 99%

Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Bhairam¹,

Shukla²,

Gidwani³

et al. 2022

IJPQA

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“…[2] As a result, the ability to generate and maintain a supersaturated condition has made amorphous solid dispersions more appealing. [4] It's a new anti-anginal drug that belongs to the piperazinacetamide family: Ranolazine is a 2-[2-hydroxy-3-(2methoxyphenoxy) propyl piprazine-1-yl]acetamide. [5] It's used for those with chronic angina who haven't responded well to other anti-anginal medications.…”

Section: Introductionmentioning

confidence: 99%

Enhanced solubility and bioavailability of ranolazine by solid dispersion method in vitro and in vivo evaluation

Bhairam

Pandey

Shukla

et al. 2022

ijhs

Self Cite

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Objective: This study aims to formulate solid dispersions incorporating ranolazine to enhance its aqueous solubility. Methodology: The poor aqueous solubility and permeability of BCS class II drug hamper their bioavailability when orally or topically administered. The present research study focused on formulating amorphous solid dispersions of ranolazine. The hydrophilic polymeric carriers like, HPMC, PEG 6000 and PVPK 30K, Soluplus were used in different ratio. Solid dispersions were prepared by employing modified solvent evaporation method. The prepared physical mixtures and solid dispersions were physico-chemically characterized using fourier transform infrared spectroscopy, scanning electron microscopy, powder x-ray diffractometry, drug content estimation by UV-spectrophotometric method. Result: Functional evaluation of ranolazine solid dispersions was carried out by solubility analysis, in-vitro dissolution studies and pharmacokinetics study. According to solubility studies, Soluplus showed the highest solubility profile among the polymers tested. An optimized ranolazine containing solid dispersions formulation composed of Soluplus at 1:2.5 ratio had 10 fold (41.21 ± 0.35μg/mL) higher solubility and dissolution over that of pure ranolazine (~ 3.92 ± 0.06μg/mL) and physical mixture (~ 4.51 ± 0.32μg/mL). In-vitro dissolution studies revealed that there was increase in solubility of drug and enhanced dissolution rate in solid dispersions compared to physical mixtures respectively.

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“…The anti-inflammatory drug has been widely used in the treatment of several diseases due to their effectiveness in relieving pain [3]. However, their sides effects limited their use, This is the reason why research focused, for long time, on the use of intelligent materials and biodegradable polymers [4,5], in order to developed an appropriate systems to carry drugs and controlled their release [6,7].…”

Section: Introductionmentioning

confidence: 99%

“…The combination between various polymeric network structure is needed to enhance the surface properties of the developed system [22]. Several studies have been carried out using chitosan and PAA due to their pH and thermo-sensitivity [6,23,24] The swelling behavior and the inter and intra molecular interactions between the polymeric chains and the surrounding medium allowed to controlled drug release and minimize their side effects.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Poly (Acrylic Acid)- Co-Chitosan Nanoparticles as pH-Thermo-Responsive System to Control Delivery

Derbali

Bouzid

Boyron³

2022

J. Basic Appl. Sci.

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The present study aims to develop a pH thermosensitive nanocarriers as a drug delivery system to better controll drug release. Nanoparticles was developed by the combination of smart polymers, chitosan and poly(acrylic acid) were chosen as biodegradable vectors to encapsulate and transport the drug. The used method was based on the polymerization of acrylic acid using reticulated chitosan as a template. Analysis of particle size, Zeta potential, and size distribution revealed that most of the resulting nanoparticles had an average diameter less than 100nm, with a high Zeta potentiel about -29.7 mV and a narrow size distribution. In addition, the developed system showed an encapsulation efficiency around 97%. In vitro release test was achieved using different buffer solutions with pH equal to 1.2, 3.6, 4.2, 4.8, 6.8 and 7.4. The release profiles showed that nanoparticles provide drug protection at different pH values. They responded at pH = 3.6 and provided sustained controlled release of up to 62.62% over 8 hours. The results reveal that the prepared nanoparticles can be used as drug delivery carriers. They can improve therapeutic efficiency of the drugs used in the treatment of inflamed tissues where the pH is around 3.6 as in the Crohn disease.

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Colloidal and vesicular delivery system for herbal bioactive constituents

Cited by 29 publications

References 136 publications

Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Enhanced solubility and bioavailability of ranolazine by solid dispersion method in vitro and in vivo evaluation

Formulation and Characterization of Poly (Acrylic Acid)- Co-Chitosan Nanoparticles as pH-Thermo-Responsive System to Control Delivery

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