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AAPS PharmSciTech ; 22(5): 201, 2021 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-34231193


Particle engineering of excipients, at sub-particulate level using co-processing, can provide high functionality excipients. NanoCrySP technology has been recently explored as a novel approach for the generation of nanocrystalline solid dispersion of poorly soluble drugs, using spray drying process. The purpose of the present study was to generate co-processed mannitol and sorbitol (SD-CSM) using NanoCrySP technology having similar composition to commercial co-processed excipient (Compressol® SM, CP). The characterization of excipients was performed to evaluate their various physicomechanical properties. The sub-micron crystallite size of sorbitol in the matrix of mannitol was determined using the Williamson-Hall equation and Halder-Wagner equation. The reduction in crystallite size of sorbitol and mannitol, lower melting point, and lower heat of fusion of SD-CSM could be responsible for excellent compactibility, better tabletability, and comparable compressibility with respect to CP. This was confirmed by the compressibility-tabletability-compactibility (CTC) profile and Heckel plot analysis. Overall, SD-CSM generated using NanoCrySP technology improved functionalities of excipients over CP and would be useful for direct compression application.

Composição de Medicamentos/métodos , Manitol/química , Nanotecnologia , Sorbitol/química , Força Compressiva , Cristalização , Excipientes/química , Tamanho da Partícula , Porosidade , Comprimidos/química , Resistência à Tração , Molhabilidade
Drug Discov Today ; 2021 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-34265460


The barrier function of skin and non-optimal physicochemical properties of drug present a challenge to skin penetration of many drugs, thus motivating the development of novel drug delivery systems. Recently, nanocrystal-based formulations have been investigated for topical drug delivery and demonstrated improved skin penetration. This review highlights barriers in skin penetration, current techniques to improve topical delivery and application of nanocrystals in conquering obstacles for topical delivery. Nanocrystals can improve delivery through the skin by mechanisms like higher concentration gradient across skin resulting in increased passive diffusion, hair follicle targeting, diffusional corona and adhesion to skin. This would be of interest for formulation scientists for product development of molecules that are 'difficult-to-deliver' topically.

Expert Opin Drug Deliv ; 18(7): 907-928, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33412936


INTRODUCTION: Polymers have various applications such as binder, film coating agent, stabilizer, drug release modification, and as primary packaging materials. Recently, they have been explored in co-processing technique to improve the functionality of small molecule excipients (SMEs). Co-processing is a concept wherein two or more excipients interact at sub-particle level to provide synergy in functionality and minimize drawbacks of individual excipients. AREA COVERED: The present review highlights the application of co-processing to improve the functionality of SMEs using polymers; physicochemical and mechanical properties of polymers for co-processing; advantages of co-processed excipients for different applications; functionality enhancement of co-processed excipients; novel concepts/methods for co-processing; mechanistic insights on co-processing and commercial products available in the market. EXPERT OPINION: Most of the SMEs do not possess optimal multifunctional properties like flow, compressibility, compactibility, and disintegration ability, required to compensate for poorly compactable drugs. Some of these drawbacks can be overcome by co-processing of SMEs with polymers. For example, co-processing of a brittle SME and plastic material (polymer) can provide a synergistic effect and result in the generation of single entity multi-functional excipient. Besides, novel co-processed excipients generated using combinations of SMEs and polymers can also generate intellectual property rights.

Excipientes , Polímeros , Liberação Controlada de Fármacos , Comprimidos
Drug Deliv Transl Res ; 11(3): 966-983, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32588281


Nanocrystals can enhance skin penetration of drug by increased saturation solubility, dissolution rate and adhesion on the skin. Apremilast is 'difficult-to-deliver' in viable layers (epidermis, dermis) and stratum corneum (SC) owing to its poor aqueous solubility and modest lipophilicity, respectively. Apremilast is currently available as oral tablet formulation for the indication of psoriasis but its effectiveness is limited by systemic side effects. Therefore, the present study aimed to develop novel nanocrystal-based formulations of apremilast for improved topical delivery. Nanosuspension was prepared using wet media milling and exhibited a mean particle size of 200 nm. The saturation solubility of nanocrystals was improved by 2-fold than micronized apremilast and showed significant advantage during dissolution study. Nanosuspension and micronized apremilast was incorporated into gel and cream and characterized for rheological properties. Skin permeation and ex vivo dermatokinetic study of topical formulations were performed on pig ear skin at a dose of 1% w/w using Franz diffusion cells. Skin permeation studies indicated that non-detectable amount of apremilast permeated through pig ear skin during exposure of formulations. Nanosuspension showed 2.6- and 3.2-fold drug penetration in SC and viable layers, respectively, over microsuspension. Nanogel showed 2.7- and 2.4-fold drug penetration in SC and viable layers, respectively, over microgel. Nanocream showed 1.2- and 2.8-fold drug penetration in SC and viable layers, respectively, over microcream. Thus, nanocrystal-based formulations of apremilast aid in selective delivery into viable layers by crossing the SC barrier. This is of paramount importance in enhancing therapeutic effectiveness utilizing localized delivery and provides an alternative delivery approach for the treatment of psoriasis. Graphical abstract.