The Solubility-Permeability Interplay for Solubility-Enabling Oral Formulations

Nainwal, Nidhi; Singh, Ranjit; Jawla, Sunil; Saharan, Vikas Anand

doi:10.2174/1389450120666190717114521

Cited by 10 publications

(6 citation statements)

References 100 publications

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“…The majority of medications in the pharmaceutical industry today have poor solubility. Poor solubility has been effectively addressed by a number of solubility enhancement strategies [6].…”

Section: Bcs Classification Systemmentioning

confidence: 99%

A review on solubility enhancement technique for pharmaceutical drugs

Vaishnavi B. Borgaonkar,

Chetan M. Jain,

Amit R. Jaiswal

et al. 2024

GSC Biol. Pharm. Sci.

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Solubility, a critical parameter governing the bioavailability and therapeutic efficacy of pharmaceutical compounds, often poses a significant challenge in drug development. This review article offers a thorough examination of several methods used to improve the solubility of medications that have low solubility, in order to overcome their limits. The discussion encompasses both conventional and emerging strategies, highlighting their mechanisms, advantages, and limitations. The study examines conventional methods such as particle size reduction, solid dispersion, and cosolvency, focusing on their historical importance and extensive use. Advances in nanotechnology, including nanosuspensions, nanocrystals, and lipid-based nanocarriers, are discussed for their potential to revolutionize solubility enhancement through improved drug delivery systems. An essential determinant in achieving optimal medication dosage absorption into the circulatory system is the demonstration of a pharmacological action is directly linked to the solubility of a substance. The primary challenge in formulating the new medicinal chemical is its limited water solubility. Medications with low solubility in water need large doses in order to achieve their highest effective concentration in the bloodstream when taken orally. The biopharmaceutical categorization system (BCS) classifies substances according to their solubility and permeability. Regulatory agencies and health organizations have used this categorization approach to validate bioequivalence for chemicals that are both highly soluble and very permeable by using dissolution as a form of confirmation. Medications that have a poor capacity to dissolve in water have a slow pace of breaking down, which results in a reduction in the amount of the medication that may be absorbed into the bloodstream when taken orally.

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“…The majority of medications in the pharmaceutical industry today have poor solubility. Poor solubility has been effectively addressed by a number of solubility enhancement strategies [6].…”

Section: Bcs Classification Systemmentioning

confidence: 99%

A review on solubility enhancement technique for pharmaceutical drugs

Vaishnavi B. Borgaonkar,

Chetan M. Jain,

Amit R. Jaiswal

et al. 2024

GSC Biol. Pharm. Sci.

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show abstract

“…The dissolution process is the rate-controlling step in BCS class II drugs due to their low solubility. 2,4,[7][8][9][10] Hypertension is a dangerous cardiovascular event resulting in an increase in arterial blood pressure. There are many medications available to treat hypertension in conventional dosage forms, but the majority of antihypertensives have low bioavailability because they are poorly water soluble.…”

Section: Introductionmentioning

confidence: 99%

Formulation of Candesartan Cilexetil Nanoparticles by Ionotropic Gelation Method Using Ultrasonication

Bisht¹,

Bolmal²,

Nainwal³

2023

Ind. J. Pharm. Edu. Res.

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Aim: Candesartan Cilexetil (CC) is a common drug used by patients suffering from hypertension and heart diseases. However, CC has poor oral bioavailability as it belongs to Biopharmaceutical Classification System (BCS) class II and has low aqueous solubility. This research work is focused to enhance the Bioavailability of CC using nanotechnology. Therefore, CC nanoparticles were developed using the ionic gelation procedure and ultrasonication. Materials and Methods: This work is aimed to formulate CC-alginate nanoparticles using the ionic gelation method and to investigate the influence of ultrasonication on the particle size and stability of nanoparticles. This work is also focused on the use of polysaccharides (sodium alginate) for nanoparticle preparation by ionic gelation technique using a cross-linking agent (calcium chloride). The physico-chemical properties, morphology, and effect of ultrasonication on particle size, as well as the effect of polymer concentration on particle size and drug release, of CC nanoparticles, were investigated. Results and Discussion: The prepared CC nanoparticles, were stable and have mean particle sizes ranging from 210-538 nm. The encapsulation efficiency of the prepared nanoparticles was reported between 67-83%. The optimized formulation was tested for its physical stability at 8°C and 25°C for 3 months. Pluronic F-68 (PF-68) was also found to have a crucial role in the long-term stability of the formulation. It was observed that sodium alginate played a pivotal role in providing sustained drug release up to 24 hr from the formulation. Conclusion: The results suggested that ultrasonication and polymer concentration leads to variation in the particle size and the homogeneity of the system.

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“…An IPN can be differentiated from a polymer blend since it swells but fails to dissolve in solvents and suppressed creep and flow deformations. 3,4 They differ from polymer complexes and graft copolymers as well, which either involve chemical bonding and a limited degree of cross-linking. IPN can be broadly referred to as "polymer alloys", allowing polymer blends to obtain the pertinent morphology by making them chemically compatible.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Inter-Penetrating Network of Isabgol Husk Mucilage for Modified Release of Diclofenac Sodium

Ale,

Nainwal,

Butola

et al. 2023

Ind. J. Pharm. Edu. Res.

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Introduction: Diclofenac Sodium (DS), a Non-Steroidal Anti-Inflammatory Drug (NSAID) is widely used in inflammation and pain management. However, the drug has a short half-life of 1.2-2 hr therefore, frequent administration of DS is required. In this research paper Inter-Penetrating Network (IPN) microspheres of Diclofenac sodium were made using Isabgol husk mucilage and Polyvinyl Alcohol (PVA) to prolong the release of diclofenac sodium. Isabgol husk is widely explored as a natural, economical, biocompatible, and biodegradable polymer for the development of a modified-release drug delivery system. Materials and Methods: IPN microspheres were prepared using Isabgol husk mucilage and Polyvinyl alcohol by emulsion cross-linking method in the presence of DL glyceraldehyde as a cross-linker. Evaluation: Fourier Transform Infrared (FTIR) spectroscopy was performed to confirm the formation of an interpenetrating network. The chemical stability of the drug and its molecular dispersion in the IPN was validated by X-ray Diffraction (XRD) analysis. The prepared microspheres were evaluated for % yield, drug loading, entrapment efficiency, surface morphology, swelling index and in vitro drug release. Results: The percentage yield and drug entrapment efficiency of the formulations were found in between 66.33 to 95.345%, and 40.24 to 68.12% respectively. The SEM and light microscopy studies confirmed the formation of spherical IPN microspheres. The model kinetics of in vitro release data found Korsmeyer-Peppas as the best-fit model for drug release from IPN microspheres.

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The Solubility-Permeability Interplay for Solubility-Enabling Oral Formulations

Cited by 10 publications

References 100 publications

A review on solubility enhancement technique for pharmaceutical drugs

A review on solubility enhancement technique for pharmaceutical drugs

Formulation of Candesartan Cilexetil Nanoparticles by Ionotropic Gelation Method Using Ultrasonication

Formulation and Characterization of Inter-Penetrating Network of Isabgol Husk Mucilage for Modified Release of Diclofenac Sodium

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