Characterization and evaluation of varieties of microcrystalline cellulose in formulations containing lactose incompatible drugs: Influence on compactibility and drug release

Abstract

The research study provides an insight into different manufacturers’ microcrystalline celluloses (MCC) thorough characterization, comprising determination of morphology, PSD, percentage crystallinity, surface area, true density, crushing strength, and compaction behavior.

Highlights

Compaction properties of MCC vary from manufacturer to manufacturer due to source variation.

Scanning electron microscopy better elucidates differences in the morphology of various MCC grades.

The crushing strength of MCC is primarily dependent on its particle size and shape.

Ceolus KG 1000 grade of MCC demonstrated better compactibility however can retard the drug release if used in higher concentrations for low-dose drugs.

Amlodipine formulation using Emocel 50M showed very rapid drug release at 50 paddle rpm without forming a heap at bottom of the dissolution vessel.

The study indicated good compaction, crushing strength for Ceolus KG 1000 and Emocel 50 M. Different varieties of MCC exhibited consistent mean yield pressure and crushing strength irrespective of their percentage crystallinity, degree of polymerization, and moisture content. The impact of these MCC characteristics was evaluated in formulations containing high and low-dose lactose incompatible drugs. Ceolus KG 1000 showed better compressibility, crushing strength and devoid of capping when used in acyclovir (high-dose) formulation. However, drug release of amlodipine (low-dose) formulation was significantly reduced when >80 % w/w Ceolus KG 1000 used.

Amlodipine formulation with Emocel 50 M showed faster drug release. On statistical evaluation, surface area and true density were found to be significant factors for mean yield pressure and crushing strength of acyclovir formulations. PSD, true density, and bulk density were found to be significant factors affecting release of amlodipine formulations. Study showed that characteristics of Ceolus KG 1000 and Emocel 50 M are favorable for acyclovir and amlodipine formulation, respectively.

Lastly, study suggests that vendor change of MCC might be unfavorable if not evaluated properly for both formulations containing high and low-dose actives.

Materials

Torrent research center (Gandhinagar, India) provided amlodipine besylate, PSD: D (0.9): NMT 100 μm, and acyclovir PSD: D (0.9):75–150 μm, as the gift samples. Eight different varieties of MCC were obtained from three different vendors. The respective details of vendors and the respective MCC grades are FMC Biopolymer, (Avicel PH 113, Avicel PH 200), Asai Kaasei (Ceolus KG 1000, Ceolus PH 200), JRS Pharma (Emcocel 50 M, Emcocel HD 90, Vivapur PH 101 and Vivapur PH 200).

Abhijeet Upadhye, Murali Monohar Pandey, Characterization and evaluation of varieties of microcrystalline cellulose in formulations containing lactose incompatible drugs: Influence on compactibility and drug release, International Journal of Biological Macromolecules, 2025, 144952, ISSN 0141-8130, https://doi.org/10.1016/j.ijbiomac.2025.144952.