scholarly journals Enhancement of solubility of poorly soluble drugs by solid dispersion: An Overview

2017 ◽  
Vol 5 (04) ◽  
pp. 17-23
Author(s):  
Katta Manogna ◽  
P. Nagaveni ◽  
K. Thyagaraju
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Drug Solubility ◽  
Solid Dosage Forms ◽  
Preparation Methods ◽  
Solid Dosage ◽  
Poorly Soluble ◽  
Poorly Water Soluble

Most of the newly invented chemical drug moieties are poorly water soluble. According to BCS classification, class II and IV drugs are considered as poorly water soluble. So enhancement of oral absorption and bioavailability of solid dosage forms remains a challenge to formulation scientists due to their solubility criteria. Therefore many techniques are being explored to enhance the solubility of poor soluble drugs. Solid dispersion is one of the most important method for enhance the solubility (dissolution rate) and hence oral bioavailability of poorly soluble drugs. In solid dispersion the particle size of drug is reduced or a crystalline pure drug is converted into amorphous form and hence the solubility is increased. Polymer incorporating in solid dispersion technology is usually hydrophilic in nature and also showing compatibility with the drug to enhance the drug solubility. This review mainly discus about solid dispersion, preparation methods, and finally characterization.

scholarly journals Solid Dispersion: Solubility Enhancement Technique of Poorly Water Soluble Drug

2020 ◽  
Vol 10 (1) ◽  
pp. 173-177 ◽  
Author(s):  
, Ikram ◽  
Kapil Kumar
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Inert Carrier ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion is a technique which is widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. Dispersion of one or more active ingredients (hydrophobic) is done with an inert carrier (hydrophilic) at solid-state prepared by fusion method, solvent, and melting solvent method. In this review article, we have focused on the methods of preparation, advantages, disadvantages and characterization of the solid dispersions. Keywords: Solid dispersion; dissolution; solubility.

scholarly journals ENHANCEMENT OF THE SOLUBILITY OF FAMOTIDINE SOLID DISPERSION USING NATURAL POLYMER BY SOLVENT EVAPORATION

2021 ◽  
pp. 193-198
Author(s):  
HUSSEIN K. ALKUFI ◽  
ASMAA M. RASHID
Keyword(s):  
Hyaluronic Acid ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Natural Polymer ◽  
Solubility Study ◽  
Poorly Soluble ◽  
Pure Drug

Objective: The aims of the study to enhance solubility and dissolution of famotidine using natural polymer. Solubility study of a drug is one of the contributing factors of its oral bioavailability. The formulation of poorly soluble drugs for oral delivery presents a challenge to the formulation technologists. Methods: The present study has shown that it is possible to raise the solubility for poorly soluble drugs like famotidine, by preparing solid dispersion using natural water-soluble polymer (xyloglucan and hyaluronic acid) as solubilizer through solvent evaporation method. Physical mixture and solid dispersion of famotidine with xyloglucan (XG) or hyaluronic acid in a ratio of 1:1, 1:2, 1:3 were prepared. Solubility study, drug content, dissolution profile and compatibility study were performed for famotidine in solid dispersions XS1, XS2, XS3, HS4, HS5, HS6 as well as in physical mixtures at a ratio 1:1 for both polymer (XG and hyaluronic acid). Results: It was observed that solid dispersions of each drugs showed an increase in dissolution rate in comparison with its pure drug in the ratio of 1:1 (Drug: carrier). It can be concluded that with the care and proper use of xyloglucan, the solubility of drugs poorly soluble can be improved. The prepared solid dispersion showed improvement of drug solubility in all prepared formulas. The best result was obtained with formula XS1 (famotidine: xyloglucan at ratio 1:1) that showed 26 fold increase in solubility compared to the solubility of pure drug. Conclusion: The natural solid dispersion, increased wettability and reduced crystallinity of the drug which leads to improving solubility and dissolution.

Encapsulation of lipid-based formulations in porous carriers for controlled drug delivery

2021 ◽  
Vol 28 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Thao T.D. Tran
Keyword(s):  
Porous Materials ◽  
Controlled Drug Release ◽  
Water Soluble ◽  
Solid Dosage Forms ◽  
Pharmaceutical Ingredients ◽  
Solid Dosage ◽  
Water Soluble Drugs ◽  
Porous Carriers ◽  
Poorly Water Soluble ◽  
And Control

: Lipid-based formulations have recently been investigated as a promising approach to enhance the bioavailability of drugs, especially poorly water-soluble drugs. The encapsulation of lipid-based formulations in porous materials can result in a transformation of liquids or semisolid forms to solid dosage forms. Moreover, the specific structure of porous carriers could offer an enhanced ability to load and control active pharmaceutical ingredients. Although there have been prominent reports on lipid-based formulations and porous materials as promising technologies for controlled drug release, the overall methods of encapsulating lipid-based formulations need to be discussed for further formulation investigations. This review aims to present the key strategies used for producing porous carriers containing lipid-based formulations. We also discuss methods that enhance the encapsulation efficiency of loaded drugs within porous structures (instead of lipid-based formulations). Moreover, the critical factors that affect tablet formation are outlined. This overview of lipid-based formulations encapsulated within porous materials provides a summary of the technical methods used in the development of these formulations and their clinical translation.

Development of an Oral Curcumin Nanocrystal Formulation

2012 ◽  
Vol 3 (4) ◽  
Author(s):  
R. Ravichandran
Keyword(s):  
The Body ◽  
Dissolution Behavior ◽  
Poorly Soluble Drugs ◽  
Solid Dosage Forms ◽  
Bioavailability Enhancement ◽  
Solid Dosage ◽  
Rapid Dissolution ◽  
Poorly Soluble ◽  
Drug Nanocrystal ◽  
Spray Dried

During the last ten years, the formulation of drugs as nanocrystals has rapidly evolved into a mature drug delivery strategy, with currently five products on the market. The major characteristic of these systems is the rapid dissolution velocity, enabling bioavailability enhancement after oral administration. This study describes the preparation of a solid dosage capsule form of spray-dried curcumin nanocrystal and compares its dissolution behavior with market capsule in different media. The aim was to obtain a stable nanocrystal loaded drug capsule with an increased drug saturation solubility and dissolution velocity. The solubility and dissolution experiments were performed to verify the obvious improvement of the dissolution behavior compared with commercial product. Improved dissolution behavior in drug nanocrystal-loaded solid dosage forms should lead to better bioavailability of poorly soluble drugs in the body.

scholarly journals Development and Characterization of the Solvent-Assisted Active Loading Technology (SALT) for Liposomal Loading of Poorly Water-Soluble Compounds

Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 465 ◽  
Author(s):  
Griffin Pauli ◽  
Wei-Lun Tang ◽  
Shyh-Dar Li
Keyword(s):  
Small Volume ◽  
Water Solubility ◽  
Water Soluble ◽  
Drug Solubility ◽  
Active Loading ◽  
Rapid Loading ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Formulation Stability

A large proportion of pharmaceutical compounds exhibit poor water solubility, impacting their delivery. These compounds can be passively encapsulated in the lipid bilayer of liposomes to improve their water solubility, but the loading capacity and stability are poor, leading to burst drug leakage. The solvent-assisted active loading technology (SALT) was developed to promote active loading of poorly soluble drugs in the liposomal core to improve the encapsulation efficiency and formulation stability. By adding a small volume (~5 vol%) of a water miscible solvent to the liposomal loading mixture, we achieved complete, rapid loading of a range of poorly soluble compounds and attained a high drug-to-lipid ratio with stable drug retention. This led to improvements in the circulation half-life, tolerability, and efficacy profiles. In this mini-review, we summarize our results from three studies demonstrating that SALT is a robust and versatile platform to improve active loading of poorly water-soluble compounds. We have validated SALT as a tool for improving drug solubility, liposomal loading efficiency and retention, stability, palatability, and pharmacokinetics (PK), while retaining the ability of the compounds to exert pharmacological effects.

Pharmacosomes as Drug Delivery System: An Overview

2021 ◽  
pp. 122-127
Author(s):  
Nikita D. Gidde ◽  
Indrayani D. Raut ◽  
Manojkumar M. Nitalikar ◽  
Shrinivas K. Mohite ◽  
Chandrakant S. Magdum
Keyword(s):  
Chemical Structure ◽  
Complex Form ◽  
Colloidal Dispersions ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Phospholipid Ratio ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
The Cost ◽  
Harmful Effects

Pharmacosomes are the colloidal dispersions of drugs covalently bound to lipids and can exist, depending on the chemical structure, as ultrafine vesicular, micellar, or hexagonal aggregates. Because of the linking of a drug (pharmakon) to a carrier (soma), they are rightly termed "pharmacosomes."Pharmacosomes can be characterized as a neutral molecule with both positive and negative charges, water-loving and fat-loving characteristics, and in complex form, an ideal polyphenol-to-phospholipid ratio. Pharmacosomes are amphiphilic lipid vesicular systems that have demonstrated their ability to increase the bio-accessibility of poorly water-soluble and poorly lipophilic medicines. Drug pharmacosomes provide an effective method of delivering the drug directly to the infection site, which contributes to a lowering in drug toxicity without harmful effects, and also lowers the cost of therapy by improving the drug's bioavailability, particularly in the case of poorly soluble drugs. Pharmacosomes are appropriate to incorporate both hydrophilic and lipophilic drugs. Pharmacosomes have been designed for multiple anti-inflammatory medications that are non-steroidal, neurological, and antineoplasty.

scholarly journals DEVELOPMENT OF NANOCRYSTAL FORMULATION WITH IMPROVED DISSOLUTION

2018 ◽  
Vol 8 (5) ◽  
pp. 118-129 ◽  
Author(s):  
Jaspreet Kaur Saini ◽  
Sandeep Kumar
Keyword(s):  
Dissolution Rate ◽  
Surface Area ◽  
Therapeutic Index ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Pharmaceutical Applications ◽  
Interesting Approach ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
The One

With the advancement in modern pharmaceutical technologies, Nanotechnology is the one of the most establish technology which is used to improve the therapeutic index and to overcome the formulation challenges of poorly water-soluble compounds. Nanocrystals, in nano range, is the interesting approach for poorly soluble drugs. Due to the small size, increased surface area enhanced the dissolution rate and solubility of drug. In this paper, current technologies and methods in nanocrystal preparation, stabilization, pharmaceutical applications and limitations of nanocrystal are reviewed. Keywords: Nanocrystal, limitations, stabilization, preparation, applications

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