Solubility Enhancement of Poorly soluble Drugs by using
Novel Techniques : A Comprehensive Review

Mahapatra, Abikesh Prasada Kumar; Vinod, Patil; Patil, Ravindra

doi:10.20902/ijptr.2019.130211

Cited by 8 publications

(4 citation statements)

References 8 publications

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“…In most circumstances, low solubility is related to poor bioavailability [1]. Improvement in solubility and increasing the rate of dissolution are fundamental techniques concerned with the medication bioavailability issues of drugs [2]. Micronization, which results in mean particle sizes of roughly 3-5 µm, is a simple approach for improving the dissolving velocity by increasing the surface area of the powdered drug.…”

Section: Introductionmentioning

confidence: 99%

Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation

Sarwar,

Iqbal,

Jamil

et al. 2023

Molecules

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Making nanoscale drug carriers could boost the bioavailability of medications that are slightly water soluble. One of the most promising approaches for enhancing the chemical stability and bioavailability of a variety of therapeutic medicines is liquid nanocrystal technology. This study aimed to prepare nanocrystals of mangiferin for sustained drug delivery and enhance the pharmacokinetic profile of the drug. The fractional factorial design (FFD) was used via a selection of independent and dependent variables. The selected factors were the concentration of mangiferin (A), hydroxypropyl methyl cellulose (HPMC) (B), pluronic acid (C), tween 80 (D), and the ratio of antisolvent to solvent (E). The selected responses were the particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency. The nanocrystals were further evaluated for mangiferin release, release kinetics, Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), particle size, zeta potential, and scanning electron microscopy (SEM). The stability studies of developed nanocrystals were performed for 6 months and pharmacokinetics on albino rabbits. The value of entrapment efficiencies ranged from 23.98% to 86.23%. The percentage release of mangiferin varied from 62.45 to 99.02%. FTIR and DSC studies showed the stability of mangiferin in the nanocrystals. The particle size of the optimized formulation was almost 100 nm and −12 mV the value of the zeta potential. The results of stability studies showed that the nanocrystals of mangiferin were stable for a period of six months. The peak plasma concentration of mangiferin from nanocrystals and suspension of mangiferin were 412 and 367 ng/mL, respectively. The value of AUC0−t of nanocrystals and suspension of mangiferin was 23,567.45 ± 10.876 and 18,976.12 ± 9.765 µg×h/mL, respectively, indicating that the nanocrystals of mangiferin showed greater availability of mangiferin compared to the suspension of the formulation. The developed nanocrystals showed a good release pattern of mangiferin, better stability studies, and enhanced the pharmacokinetics of the drug.

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Section: Introductionmentioning

confidence: 99%

Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation

Sarwar,

Iqbal,

Jamil

et al. 2023

Molecules

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show abstract

“…Approximately 40% of pharmaceutical products in the market are of poorly water-soluble drugs [2,3]; therefore, many studies have been performed to improve the solubilization of drugs through techniques, such as size reduction, salt formation, solid dispersion, hot-melt extrusion, or formation of salt, prodrugs, and co-crystals. Alternatively, the utilization of self-nanoemulsifying drug delivery system (SNEDDS) self-microemulsifying drug delivery system (SMEDDS), nanoemulsions and micelles has also been reported [4][5][6][7][8].…”

Section: Introductionmentioning

confidence: 99%

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

2021

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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.

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“…The transformation of the crystalline drug to an amorphous drug upon SD formulation increases the dissolution rate. 4 SD techniques have been used to increase the solubility of a poorly water-soluble drug. SD is a viable and economical method to enhance the bioavailability of poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis

Rao¹,

Paul²

2021

J. Drug Delivery Ther.

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The aim of this study was to prepare mucoadhesive vaginal tablets of clotrimazole for treatment of vaginal candidiasis. A combination of mucoadhesive polymers like HPMC K100M, Sodium CMC, and Eudragit L100 were used in different ratios prepare solid dispersions to enhance its solubility. Tablets were prepared by the wet granulation method. Solid dispersions were evaluated for saturation solubility. All tablet batches were evaluated for weight variation, hardness, friability, drug content, swelling index, in vitro drug release study, ex vivo diffusion and mucoadhesive strength. FTIR spectra showed there was no interaction between the drug and the excipients. HPMC K100 M increased the solubility of clotrimazole in simulated vaginal fluid at pH 4.5. Eudragit L100 was shown to increase the swelling and mucoadhesive strength of the tablet, i.e., 3.03 and 3.29 g. The in vitro and ex vivo release of all 9 batches showed between 61 to 78% release in 8h. Ex vivo diffusion studies using sheep vaginal membrane showed 43 to 59% in 6h in simulated vaginal fluid. The release and flux were nearly comparable to marketed tablet i.e., Candid-V6. The drug release of all batches followed the Korsmeyer-Peppas kinetic model, and the mechanism was found to be non‐Fickian/anomalous. Keywords: Clotrimazole, solid dispersion, HPMC K100M, Eudragit L100, Sodium CMC.

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Solubility Enhancement of Poorly soluble Drugs by using Novel Techniques : A Comprehensive Review

Cited by 8 publications

References 8 publications

Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation

Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation

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

Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis

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