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Research on the Prediction and Optimization of the Solubility and Permeability of Biopharmaceuticals

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Dear Colleagues,

The Biopharmaceutical Classification System (BCS) is widely used by both regulatory agencies and the pharmaceutical industry. This classification considers the solubility and permeability of drugs. The development of in vitro biopredictive methods for estimating the solubility and permeability of pharmaceutical formulations is a topic of general interest, particularly in recent years. The formulation of pharmacological molecules in conjunction with solubility enhancers and intestinal permeability enhancers is common practice today. These methods are especially useful for the optimization of these formulations before advancing to later stages of the drug development process. This can help provide patients with safer, effective, and high-quality medication in less time and at a lower cost.

In this Special Issue, we aim to highlight recent advances in drug formulation development and biopredictive tools to analyze liberation and absorption processes. We welcome original research and review articles highlighting the latest advances in dissolution and permeability tests.

We look forward to receiving your contributions.

Prof. Dr. Marta González-Álvarez
Prof. Dr. Isabel Gonzalez-Alvarez
Dr. Alejandro Ruiz-Picazo
Guest Editors

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Keywords

biopredictive test
drug delivery systems
in vitro/in vivo studies
drug development
generic industry
dissolution test
absorption
permeability
biowaivers

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Research

15 pages, 2181 KiB

Open AccessArticle

In Vivo Relevance of a Biphasic In Vitro Dissolution Test for the Immediate Release Tablet Formulations of Lamotrigine

by Tuba Incecayir and Muhammed Enes Demir

Pharmaceutics 2023, 15(10), 2474; https://doi.org/10.3390/pharmaceutics15102474 - 17 Oct 2023

Viewed by 1275

Abstract

Biphasic in vitro dissolution testing is an attractive approach to reflect on the interplay between drug dissolution and absorption for predicting the bioperformance of drug products. The purpose of this study was to investigate the in vivo relevance of a biphasic dissolution test for the immediate release (IR) formulations of a Biopharmaceutics Classification System (BCS) Class II drug, lamotrigine (LTG). The biphasic dissolution test was performed using USP apparatus II with the dual paddle modification. A level A in vitro-in vivo correlation (IVIVC) was constructed between the in vitro partition into the octanol and absorption data of the reference product. A good relation between in vitro data and absorption was obtained (r² = 0.881). The one-compartment open model was introduced to predict the human plasma profiles of the test product. The generic product was found to be bioequivalent to the original product in terms of 80–125% bioequivalence (BE) criteria (85.9–107% for the area under the plasma concentration curve (AUC) and 82.7–97.6% for the peak plasma concentration (C_max) with a 90% confidence interval (CI)). Overall, it was revealed that the biphasic dissolution test offers a promising ability to estimate the in vivo performance of IR formulations of LTG, providing considerable time and cost savings in the development of generic drug products. Full article

(This article belongs to the Special Issue Research on the Prediction and Optimization of the Solubility and Permeability of Biopharmaceuticals)

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18 pages, 6069 KiB

Open AccessArticle

Topical Micro-Emulsion of 5-Fluorouracil by a Twin Screw Processor-Based Novel Continuous Manufacturing Process for the Treatment of Skin Cancer: Preparation and In Vitro and In Vivo Evaluations

by Ajinkya Nitin Nikam, Angela Jacob, Ruchira Raychaudhuri, Gasper Fernandes, Abhijeet Pandey, Vinay Rao, Sheikh F. Ahmad, Ananth S. Pannala and Srinivas Mutalik

Pharmaceutics 2023, 15(9), 2175; https://doi.org/10.3390/pharmaceutics15092175 - 22 Aug 2023

Cited by 1 | Viewed by 1235

Abstract

5-Fluorouracil (5-FU), a BCS class III drug, has low oral bioavailability and is cytotoxic in nature causing severe systemic side effects when administered through the intravenous route. Topical drug delivery could potentially mitigate the systemic side-effects. Microemulsions (MEs) would be an apt solution due to enhanced partitioning of the drug to the skin. However, conventional methods for preparing MEs are inefficient since they are not continuous and are very tedious and time-consuming processes hence revealing the need for the development of continuous manufacturing technology. In our study, 5-FU MEs were prepared using a continuous manufacturing Twin Screw Process (TSP) and its efficiency in the treatment of skin cancer was evaluated. Water-in-oil MEs were prepared using isopropyl myristate as the oil phase and Aerosol OT and Tween 80 as the surfactants. The average particle size was observed to be 178 nm. Transmission electron microscopy was employed to confirm the size and shape of the MEs. FTIR study proved no physical or chemical interaction between the excipients and the drug. In vitro drug release using vertical diffusion cells and ex vivo skin permeation studies showed that the drug was released sustainably and permeated across the skin, respectively. In in vitro cytotoxicity studies, 5-FU MEs were accessed in HaCat and A431 cell lines to determine percentage cell viability and IC50. Skin irritation and histopathological examination implied that the 5-FU MEs did not cause any significant irritation to the skin. In vivo pharmacodynamics studies in rats suggested that the optimised formulation was effective in treating squamous cell carcinoma (SCC). Therefore, 5-FU MEs efficiently overcame the various drawbacks faced during oral and intravenous drug delivery. Also, TSP proved to be a technique that overcomes the various problems associated with the conventional methods of preparing MEs. Full article

(This article belongs to the Special Issue Research on the Prediction and Optimization of the Solubility and Permeability of Biopharmaceuticals)

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